- The dissociation chemistry of low-energy N-formylethanolamine ions: Hydrogen-bridged radical cations as key intermediates
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Tandem mass spectrometry experiments show that N-formylethanolamine molecular ions HOCH2CH2NHC(H)O+ (FE1) lose C2H3O, CH2O and H2O to yield m/z 46 ions HC(OH)NH2+, m/z 59 ions CH2N(H)CHOH +, and m/z 71 N-vinylformamide ions CH2C(H)N(H)CHO +. A detailed mechanistic study using the CBS-QB3 model chemistry reveals that the readily generated 1,5-H shift isomer HOCHCH2N(H)C(H) OH+ (FE2) and hydrogen-bridged radical cations (HBRCs) act as key intermediates in a 'McLafferty + 1′ type rearrangement that yields the m/z 46 ions. The co-generated C2H3O neutrals are predicted to be vinyloxy radicals CH2CHO in admixture with CH3CO generated by quid-pro-quo (QPQ) catalysis. A competing C-C bond cleavage in FE1 leads to HBRC [CH2N(H)C(H)O-...H...OCH2] +, which serves as the direct precursor for CH2O loss. In addition, ion FE2 also communicates with a myriad of ion-molecule complexes of vinyl alcohol and formimidic acid whose components may recombine to form distonic ion FE3, HOCH(CH2)N(H)C(H)OH+, which loses H 2O after undergoing a 1,5-H shift. Further support for these proposals comes from experiments with D- and 18O-labelled isotopologues. Previously reported proposals for the H2O and CO losses from protonated N-formylethanolamine are briefly re-examined.
- Jobst, Karl J.,Bowen, Richard D.,Terlouw, Johan K.
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Read Online
- Toward the design of LPEI containing block copolymers: Improved synthesis protocol, selective hydrolysis, and detailed characterization
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The synthesis of poly(2-ethyl-2-oxazoline)-b-linear poly(ethylenimine) (PEtOx-b-LPEI) copolymers by selective basic hydrolysis of PEtOx-b-poly(2-H-2- oxazoline) (PEtOx-b-PHOx) is described. For this purpose, an easy method for the preparation of the 2-H-2-oxazoline (HOx) monomer was developed. Based on the microwave-assisted polymerization kinetics for this monomer, PEtOx-b-PHOx copolymers were prepared. Subsequently, the block copolymers were selectively hydrolyzed to PEtOx-b-LPEI under basic conditions. The success of the polymerizations and subsequent post-polymerization reactions was demonstrated by 1H NMR spectroscopy and MALDI-TOF-MS investigations of the obtained polymers.
- Tauhardt, Lutz,Kempe, Kristian,Schubert, Ulrich S.
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Read Online
- ALPHA-HELIX MIMETIC WITH FUNCTIONALIZED PYRIDAZINE
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The synthesis of new α-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available dimethyl pyridazine-3,6-dicarboxylate building block. These scaffolds may be thought of as synthetic counterparts of amphiphilic α-helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix.
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- METHOD OF MAKING UP WITH LIGHT-SENSITIVE MAKEUP BY APPLYING A BASE LAYER AND A KIT FOR IMPLEMENTING SUCH A METHOD
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The present invention provides a method of making up human keratinous material with light-sensitive makeup, wherein: a) a base layer of a first composition is applied to the keratinous material, the first composition containing at least one optical agent that configured for, at least temporarily, of forming a screen at a wavelength λ; andb) a thermally stable photochromic second composition is applied on the base layer, the second composition being developable by exposure to a radiation at least of the wavelength λ.
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- METHOD OF MAKING UP WITH A LIGHT-SENSITIVE MAKEUP, AND A LIGHT-SENSITIVE MAKEUP COMPOSITION
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The present invention provides a method of making up human keratinous material with a light-sensitive makeup, in which: i. a layer of a thermally stable photochromic composition comprising a photochromic agent capable of being developed by UV radiation and an optical agent that screens UV radiation is applied to the keratinous material; and ii. the layer of composition is exposed in non uniform manner to UV radiation to excite the photochromic agent and create a light-sensitive makeup look, the screening power F of the composition as regards solar UV radiation (280 nm to 400 nm) being 2 or more.
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- GLYCOPROTEIN SYNTHESIS AND REMODELING BY ENZYMATIC TRANSGLYCOSYLATION
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A chemoenzymatic method for the preparation of a homogeneous glycoprotein or glycopeptide, including (a) providing an acceptor selected from the group consisting of GlcNAc-protein and GlcNAc-peptide; and (b) reacting the acceptor with a donor substrate including an activated oligosaccharide moiety, in the presence of a catalyst comprising endoglycosidase (ENGase), to transfer the oligosaccharide moiety to the acceptor and yield the homogeneous glycoprotein or glycopeptide. The donor substrate includes, in a specific implementation, a synthetic oligosaccharide oxazoline. A related method of glycoprotein or glycopeptide remodeling with a predetermined natural N-glycan or a tailor-made oligosaccharide moiety, and a method of remodeling an antibody including a heterogeneous sugar chain, are also described. The disclosed methodology enables glycoprotein drugs to be modified for prolonged half-life in vivo, reduced immunogenicity, and enhanced in vivo activity, and for targeting and drug delivery.
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- Synthesis and catalytic properties of diverse chiral polyamines
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Chiral polyamines can be utilized for a variety of potential applications, ranging from asymmetric catalysis to nonviral gene delivery systems for DNA and RNA. They can also be utilized to solubilize carbon nanotubes. Thus, methods for the straightforward synthesis of chiral polyamines are needed. We present herein two synthetic strategies for accessing chiral polyamines. The potential of these chiral amines to catalyze two organic reactions with a high degree of chiral induction was also explored.
- Levine, Mindy,Kenesky, Craig S.,Zheng, Shengping,Quinn, Jordan,Breslow, Ronald
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p. 5746 - 5750
(2008/12/22)
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- Cosmetic composition forming a tackifying coating comprising a polymer with a non-silicone skeleton and reactive functional groups
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Cosmetic compositions, comprising at least one polymer with a non-silicone skeleton, comprising at least two reactive chemical functional groups, that is capable of forming a tackifying coating on the hair, a cosmetic process comprising the application of the composition to the hair, and also its use for producing a tackifying coating on the hair.
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- Cosmetic composition forming a soft coating comprising a polymer having a non-silicone backbone and reactive functional groups
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Nontacky cosmetic compositions, such as hair compositions, comprising at least one polymer having a non-silicone backbone, comprising at least two reactive chemical functional groups, capable of forming a soft coating on hair, a cosmetic process comprising the application of this composition to hair and its use for producing a soft coating on hair.
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- Cosmetic composition forming a rigid coat, comprising a polymer with a non-silicone skeleton and containing reactive functional groups
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Cosmetic compositions, such as hair compositions, comprising at least one polymer with a non-silicone skeleton, comprising at least two reactive chemical functional groups, which are capable of forming a rigid coat on the hair, a cosmetic process comprising the application of this composition onto the hair, and its use for producing a rigid coat on the hair.
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- Ligands for chiral catalysis
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Novel phosphine oxazoline ligands of formula (I) whereinm is 1, 2, 3 or 4;n, p, q, r are independently zero or 1 provided that at least one of n, p, q and r is 1;X is O, S, Se, CH2, NH;Y is N, P, As, S;R is H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; ferrocenyl; a thioalkyl group; a thioaryl group; or R is part of a polymeric structure, for example polyacrylic acid;R1 to R13 are independently selected from H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether;a process for the preparation thereof, metal complexes containing such ligands and the use of such complexes, or combinations of ligand with metal salts or complexes, as catalysts for asymmetric syntheses is disclosed.
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- Phosphinite-oxazolines and metal complexes
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Compounds of formulae I and Ia, wherein X1 is secondary phosphino; R3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon atom, having from 2 to 20 atoms and at least one hetero atom selected from the group O, S and NR, or ferrocenyl; R is H or C1-C4alkyl; each R4 individually or both R4 together are a hydrocarbon radical having from 1 to 20 carbon atoms; and R01 and R02 are each independently of the other a hydrogen atom or a hydrocarbon radical having from 1 to 20 carbon atoms, are chiral ligands for metal complexes with metals of sub-groups I and VIII, which are catalysts for asymmetric addition reactions, for example of hydrogen, to prochiral unsaturated organic compounds.
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- ALKYLOXYAMINO SUBSTITUTED FLUORENONES AND THEIR USE AS PROTEIN KINASE C INHIBITORS
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The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).
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- Antimycobacterial agents
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Compounds represented by the formula [1] R1is H or a substituent; R2and R3are C1-C3alkyl; R4is siderophore group e.g. CH3—(CH2)n—C(O)—N(OH)—(CH2)m— with n=10-22, m=2-6; X is O, S, or NH; X1is O or NH; Y is H or alkyl; Z is H or substituted amino, e.g., t-BocNH or CbzNH, and r is 2-4; are useful in the method provided for treating tuberculosis. [1] is prepared by coupling [7], wherein HX1is HO— or H2N—, ?with [4] obtained as the free acid after saponification of the methyl ester.
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- Intermediates for making HIV-protease inhibitors
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HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.
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- Synthesis of clasto-lactacystin beta-lactone and analogs thereof
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The present invention is directed to an improved synthesis of clasto-lactacystin- beta -lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin- beta -lactones, and analogs thereof and their use as proteosome inhibitors.
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- Synthesis of paclitaxel from baccatin III by protection of the 7-hydroxyl of baccatin III using a strong base and an electrophile
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Process for synthesizing paclitaxel by treating baccatin III with a strong base in a solvent, adding an electrophile to the solution to form a 7-O-protected baccatin III derivative, reacting the 7-O-protected baccatin III derivative with a protected paclitaxel sidechain in a solvent such that the protected paclitaxel sidechain is coupled to the 13-hydroxyl of the 7-O-protected baccatin III, and subsequently deprotecting the protected paclitaxel sidechain and the 7-O protecting group to form paclitaxel, and intermediates used therein.
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- Process for preparing 4-tert-butyloxycarbonyl-(S)-piperazine-2-tert-butylcarboxamide
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An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxamide, an intermediate for an HIV protease inhibitor.
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- Chiral bisphosphines
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New chiral biphosphines, e.g., STR1 are useful as key components in catalysts for asymmetric reactions, providing desirably high enantiomeric excess (ee).
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- Antibacterial agents
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A compound represented by formula I: STR1 is disclosed. The compounds are active primarily against gram negative organisms. Pharmaceutical compositions and methods of treatment are also disclosed.
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- PROCESS FOR PREPARING 4-TERT-BUTYLOXYCARBONYL-(S)-PIPERAZINE-2-TERT-BUTYLCARBOXAMIDE
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An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxaimide, an intermediate for an HIV protease inhibitor.
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- OXAZOLINONE DERIVATIVES HAVING CYTOSOLIC PHOSPHOLIPASE A2 INHIBITORY ACTIVITY
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The present invention relates to a compound represented by the formula wherein a and b are each a carbon atom; a bond between a and b indicates that it is a single bond or a double bond; X is a hydrogen atom, an optionally substituted aryl group, an optionally substitued heteroaryl group, or an optionally substituted aralkyl group; Y is a hydrogen atom, an optionally substituted aryl group, an optionally substituted aralkyl group, or a carboxyl group or related functional groups thereof; and Z is a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted aralkyl, an optionally substituted arylalkenyl group, an optionally substituted heteroarylalkyl group, an optionally substituted heteroarylalkenyl group, an optionally substituted aryloxyalkyl group, an optionally substituted aralkyloxyalkyl group, an optionally substituted arylcarbonylalkyl group, an optionally substituted arylsulfonylalkyl group, an optionally substituted heteroarylsulfonylalkyl group, an optionally substituted aminoalkyl group, an optionally substituted carboxyalkyl group or related functional groups thereof, an optionally substituted alkyloxycarbonyl group, an optionally substituted aralkyloxycarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted alkylsulfonyl group, an optionally substituted arylsulfonyl group, or an optionally substituted heteroarylsulfonyl group; provided that X, Y and Z are not a hydrogen atom at the same time, and a pharmaceutical composition containing the same. The compounds of the present invention have a cytosolic phospholipase A2 inhibitiory activity.
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- Carbamoyl substituted heterocycles
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This invention relates to carbamoyl substituted heterocycles which are ω-phenyl-ω-(3-pyridyl)-ω-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring and which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as pharmaceutical formulations containing them, methods for their use, and processes and intermediates for their preparation.
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- PREPARATION OF SUBSTITUTED ALKENOIC ACIDS
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This invention relates to a highly selective process for preparation of E-ω-phenyl-ω-(3-pyridyl)-ω-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as to intermediates therefor.
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- Intermediates for making HIV-protease inhibitors
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HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.
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- Prostaglandin analogs
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Thromboxane receptor antagonist activity is exhibited by compounds of the formula STR1 wherein: V is --(CH 2) m --, --O--, or STR2 but if V is --O--or STR3 R 3 and R 4 must complete an aromatic ring; W is --(CH 2) 2 --, --CH CH-- or phenylene;X is a single bond, --CH CH--, --(CH 2) n --, or --O--(CH 2) n --; or X is branched alkylene or --O--branched alkylene wherein W is linked to Y through a chain n carbon atoms long;Y is --CO 2 H, --CO 2 alkyl, --CO 2 alkali metal, --CH 2 OH, --CONHSO 2 R 5, --CONHR 6, or --CH 2 -5-tetrazolyl;Z is O or NH;R 3 and R 4 are each independently hydrogen or alkyl or R 3 and R 4 together complete a ring optionally substituted through a ring carbon with a halo, lower alkyl, phenyl, halo (lower alkyl), halophenyl, oxo or hydroxyl group; and the remaining symbols are as defined in the specification.
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- PROCESS FOR PREPARING 4-TERT-BUTYLOXYCARBONYL-(S)-PIPERAZINE-2-TERT-BUTYLCARBOXAMIDE
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An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butyl-carboxamide, an intermediate for an HIV protease inhibitor.
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- Method for inhibiting the growth of mammalian cells
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A method for inhibiting mammalian cell growth is disclosed. The method uses compounds known as N-acetonylarylamides. The compounds have been shown to inhibit cell mitosis and to inhibit microtubule assembly. The method may be used to treat diseases associated with rapid cell growth, particularly cancer. The compounds used in the method of the present invention may be used in combination with other therapies and may be administered by known techniques for drug administration.
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- Preparation of substituted alkenoic acids
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This invention relates to a highly selective process for preparation of E-ω-phenyl-ω-(3-pyridyl)-ω-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as to intermediates therefor.
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- Retro-Ene Reactions in Heterocyclic Synthesis. III. A New Route to 4,5-Dihydrooxazoles and 5,6-Dihydro-4H-1,3-oxazines
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Methyl (E)-4,4-dimethyl-5-oxo-2-pentenoate (1, X = O) reacted with 1,2- or 1,3-aminoalcohols 3 to yield oxazolidines 4a-c or tetrahydro-1,3-oxazines 4d,e. The corresponding imino ester 1 (X = NBu-t) also gave 4 on reaction with 3. Compounds 4 on heating at 230° yielded 4,5-dihydrooxazoles 5a-c or 5,6-dihydro-4H-1,3-oxazines 5d,e along with methyl 4-methyl-3-pentenoale (6).
- Ito, Kunio,Miyajima, Shingo
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p. 501 - 503
(2007/10/03)
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- Process for making HIV protease inhibitors
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A process for making a clinically efficacious HIV protease inhibitor Compound J eliminates one step in its synthesis, by an improved, alternative synthesis of the 2(S)-4-picolyl-2-piperazine-t-butyl-carboxamide intermediate.
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- Process to make HIV protease inhibitor from (2S)-4-picolyl-2-piperazine-t-butylcarboxamide
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A process for making a clinically efficacious HIV protease inhibitor eliminates one step in its synthesis, by an alternative convergent synthesis using 2(S)-4-picolyl-2-piperazine-t-butylcarboxamide as an intermediate.
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- Carbamoyl substituted oxazoles as thromboxane receptor antagonists
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This invention relates to carbamoyl substituted heterocycles which are ω-phenyl-ω-(3-pyridyl)-ω-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring and which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as pharmaceutical formulations containing them, methods for their use, and processes and intermediates for their preparation.
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- Fungicides for the control of take-all disease of plants
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A method of controlling Take-All disease of plants by applying a fungicide of the formula STR1 wherein Z1 and Z2 are C and are part of an aromatic ring which is benzothiophene; and A is selected from --C(X)-amine wherein the amine is an unsubstituted, monosubstituted or disubstituted amino radical, --C(O)--SR3, --NH--C(X)R4, and --C(=NR3)--XR7 ; B is --Wm --Q(R2)3 or selected from O-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R4 ; Q is C, Si, Ge, or Sn; W is --C(R3)p H(2-p) --; or when Q is C, W is selected from --C(R3)p H(2-p), --N(R3)m H(1-m)--, --S(O)p--, and --O--; X is 0 or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R and R2 is independently defined herein; R3 is C1 -C4 alkyl; R4 is C1 -C4 alkyl, haloalkyl, alkoxy, alkylthio, alkylamino, or dialkylamino; and R7 is C1 -C4 alkyl, haloalkyl, or phenyl, optionally substituted with halo, nitro, or R4 ; or an agronomic salt thereof.
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- Reductive amination process
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A process of reductive amination efficiently yields an HIV protease inhibitor.
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- RETROVIRAL PROTEASE INHIBITING COMPOUNDS
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A retroviral protease inhibiting compound of the formula: STR1 is disclosed wherein R 1, R 2, R 5, R 6, Y m and Y' n are herein defined.
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- Regiospecific process to make cis-1-amino-2-alkanol from epoxide
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A regioselective process is disclosed for synthesis of 1R-amino-2S-indanol or 1S-amino-2R-indanol, wherein the stereochemical integrity of the carbon-oxygen bond at C-2 in the indene oxide starting material is retained.
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- BIS-HETEROCYCLIC PROSTAGLANDIN ANALOGS
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Thromboxane receptor antagonist activity is exhibited by compounds of the formula STR1 wherein: W is--(CH 2) m--or STR2 but if R. sup.3 and R 4 complete an aromatic ring, then W cannot be STR3 X is--(CH 2) 2--,--CH=CH--or phenylene; Y is--O--, a single bond or vinylene, except that Y cannot be--O--when n is 0, and if Y is vinylene, then n must be 0;Z is O or NH;R 3 and R 4 are each independently hydrogen, alkyl, alkenyl, or alkynyl, or R. sup.3 and R 4 together complete a ring as defined in the specification, optionally substituted through a ring carbon with an oxo or hydroxyl group; and the remaining symbols are as defined in the specification.
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- 7-oxabicycloheptyl substituted heterocyclic thioamide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
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7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula STR1 wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH2)2 --, --CH=CH-- or STR2 wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is STR3 then Y cannot be O, and when Z is --CH=CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO2 H, CO2 lower alkyl, CH2 OH, CO2 alkali metal, CONHSOR3, CONHR3a or --CH2 -5-tetrazolyl, X is O, S or NH; and where R1, R2, R3 and R3a are as defined herein.
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- Oligosaccharide oxazolines, oligosaccharide conjugates and methods of preparation thereof
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This invention relates to a method of producing peracetyloxazolines from peracetyl saccharides. The method involves reacting the starting material, a peracetyl saccharide, with a reagent combination, to directly produce the peracetyl oxazoline. This method may be used for the activation of oligosaccharides, wherein an oligosaccharide containing a reducing GlcNAc terminus is activated by the formation of an orazoline at the terminal GlcNAc, and then coupled with a bifunctional spacer to provide an oligosaccharide-spacer conjugate. The activated oligosaccharide-spacer conjugate is then coupled to a protein, such as granulocyte colony stimulating factor or γ-interferon, providing a neoglycoprotein conjugate. The invention provides a method for forming neoglycoprotein conjugates which may improve biological and physiochemical properties of the protein. For example, serum lifetime or efficiency of drug delivery of the peptide to a target organ or cell may be improved.
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- Stereo-selective synthesis of 2-aryl-propionic acids of high optical purity by using chiral oxazolines
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The present invention relates to a stereospecific chemical synthesis of optically pure enantiomers of 2-aryl-alkanoic acids, especially those of the biologically active (S)-aryl-propionic acids, in good chemical yields, useful for preparing large quantities thereof, and having a high optical purity.
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- Carbacyclin analogs
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Carbacyclin analogs that exhibit platelet aggregation inhibition activity and other biological activites common to structurally related prostacyclins are provided.
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- 7-oxabicycloheptyl substituted heterocyclic amide or ester prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
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7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasopastic disease have the structural formula STR1 wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH2)2 --, --CH=CH-- or STR2 wherein Y is O, a single bond or vinyl, with the proviso that when n is 0, if Z is STR3 then Y cannot be O, and Z is --CH=CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO2 H, CO2 lower alkyl, CH2 OH, CO2 alkali metal, CONHSOR3, CONHR3a or --CH2 --5-tetrazolyl, X is O, S or NH; and where R1, R2, R3 and R3a are as defined herein.
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- Condensation of Homophthalic Anhydrides with Heterocyclic Imines and DMAD under Mild Conditions
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Condensation of 7-methoxyhomophthalic anhydride with 2-imidazoline, 2-thiazoline, 2-oxazoline, 1-pyrroline trimer and DMAD (with triethylamine) occurs rapidly under mild conditions.
- Smith, Forrest T.,Atigadda, Ram V.
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p. 1813 - 1816
(2007/10/02)
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- Polymerizable pyrrolidonyl oxazoline monomers, homopolymers and copolymers
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What is described herein are polymerizable pyrrolidonyl 4,5-unsubstituted oxazoline monomers, homopolymers thereof, and copolymers with other monomers. A preferred polymerizable monomer compound is 2-(1-methyl-2-pyrrolidon-4-yl)-2-oxazoline. The polymers herein have excellent hydrotropic properties thus increasing the water solubility of organic compounds previously considered as water insoluble, and exhibit complexation with water soluble cosolutes.
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- Compounds for tagging nucleic acid probes
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Nucleic acid hybridization probes are provided which comprise an N4 -(substituted amino)cytosine moiety, wherein the substituted amino group comprises a tag moiety, whereby the probe is detected. Methods of preparing probes of the invention, intermediates used in such methods, and methods of using the probes of the invention in hybridization assays are also provided. Typical tag moieties employed with the probes of the invention are biotinyl, aminothiadiazole and fluorescein derivatives, connected to N4 -amino groups of modified cytosines of the probe through linker moieties. Probes tagged with biotin are typically detected by binding to the biotinyl moieties, through a streptavidin or avidin molecule, a reporter group which includes streptavidin or avidin and then detecting a signal due to the reporter group. Probes tagged with aminothiadiazole derivatives are typically detected by essentially the same method as those tagged with biotinyl but employing as reporter group one which binds to the derivative through a carbonic anhydrase molecule. Probes tagged with fluorescein derivatives are detected by a fluorescence spectroscopic method without binding of a reporter group to the tag.
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