- Reductive Alkylation of Amines with Carboxylic Ortho Esters
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We have demonstrated for the first time that carboxylic ortho esters could be used as an alkylating agent in the reductive alkylation of amines. A variety of amines, including amino acid esters, were alkylated affording mono-alkylated products with high selectivity in practical to high yields using standard heterogeneous catalysts. By applying acyclic ortho esters alkylation was completed at room temperature. (Figure presented.).
- Kadyrov, Renat,Moebus, Konrad
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supporting information
p. 3352 - 3357
(2020/07/04)
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- N -Monomethylation of amines using paraformaldehyde and H2
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The selective N-monomethylation of amines is an important topic in fine chemical synthesis. Herein, for the first time, we described a selective N-monomethylation reaction of amines with paraformaldehyde and H2 in the presence of a CuAlOx catalyst. A variety of amines, including primary aromatic amines, benzylamine and cyclohexylamine, as well as secondary amines, have been shown to be compatible with this reaction.
- Wang, Hongli,Huang, Yongji,Dai, Xingchao,Shi, Feng
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supporting information
p. 5542 - 5545
(2017/07/06)
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- Optimized triazine-mediated amidation for efficient and controlled functionalization of hyaluronic acid
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Triazine-based coupling agents have the potential to replace carbodiimides in the functionalization of hyaluronic acid (HA) giving derivatives with high degrees of substitution (DS) under mild conditions with excellent efficiency. Kinetics of the triazine
- Borke, Tina,Winnik, Fran?oise M.,Tenhu, Heikki,Hietala, Sami
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supporting information
p. 42 - 50
(2015/02/02)
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- A dramatic effect of the ionic liquid structure in esterification reactions in protic ionic media
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Bronsted acidic ionic liquids (ILs) have been synthesized and investigated as catalysts in esterification and transesterification reactions: simple and non-corrosive salts characterized by aliphatic cations associated with an "acidic" anion (in particular, [HSO4]-) gave the higher yields. A quite good correlation between IL acidity (H 0) and catalytic ability was found although also the hydrophilic nature of the ionic medium probably affects the process efficiency.
- Chiappe, Cinzia,Rajamani, Sunita,D'Andrea, Felicia
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p. 137 - 143
(2013/02/25)
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- Vitamin E conjugates
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Vitamin E conjugates, methods for their preparation, and compositions that include the conjugates. The vitamin E conjugates include a tocopherol moiety covalently coupled through a linker moiety to either a pyroglutamate moiety, a pyrrolidinone moiety, or a gentisic acid moiety.
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Page/Page column 8-9
(2010/02/10)
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- Novel acyl-dipeptide-like compounds bearing an accessory functional side chain spacer, a method for preparing the same and pharmaceutical compositions containing such products
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The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state. Compounds of the present invention have immunomodulating properties like adjuvants, In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targetting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.
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- Small organic molecule regulators of cell proliferation
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
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- PROCESS AND INTERMEDIATES FOR THE PREPARATION OF (1R, 2S, 5S)-3-AZABICYCLO[3, 1, 0]HEXANE-2-CARBOXAMIDE, N-[3-AMINO-1-(CYCLOBUTYLMETHYL)-2, 3-DIOXOPROPYL] ]-3-[(2S)-2-[[[1, 1-DIMETHYLETHYL]AMINO]CARBONYLAMINO]-3, 3-DIMETHYL-1-OXOBUTYL]-6, 6-DIMETHYL
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In one embodiment, the present application relates to a process of making a compound of formula (I): and to certain intermediate compounds that are made within the process of making the compound of formula (I).
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Page/Page column 22-23
(2008/06/13)
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- THE METHOD FOR PRODUCTION OF SEMI-FINISHED PRODUCTS USEFUL IN SYNTHESIS OF PACLITAXEL
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The method for production of the semi-finished products useful in synthesis of Paclitaxel with the generalized formula (2), characterized in that phenyl isoserine derivatives, or mixtures of their epimerides with various configurations on the carbon 2' or their salts, are treated with triazine type condensing agent, possible in the presence of tertiary amine, in medium of anhydrous organic solvent, and the triazine esters produced are treated with Baccatin III, in medium of anhydrous organic solvent, possible in the presence of a catalyst.
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- Novel antioxidants, preparation processes and their uses
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The invention concerns a process for preparing compounds of general formula (I) wherein R and R′ represent an alkyl radical or an aryl group; and R″ is hydrogen or a CO—R1 group wherein R1 is an alkyl radical or an aryl group; and wherein these compounds are or not in the thiazolidine form; by protecting the N-acyl-L-cysteine to form an intermediate compound; and then by coupling said intermediate compound with S-acylcysteamine hydrochloride or with thiazolidine.
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- Small organic molecule regulators of cell proliferation
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A compound represented in general formula (X) and (XI):
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- Acyl pseudodipeptides which carry a functionalised auxialiary arm
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The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state. Compounds of the present invention have immunomodulating properties like adjuvants, In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targetting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.
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- Small organic molecule regulators of cell proliferation
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
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- Metalloproteinase inhibitors, their therapeutic use and process for the production of the starting compound in the synthesis thereof
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Objects of the present invention are compounds of a peptido-mimetic character having the capacity of acting as inhibitors of metalloproteinases produced by venom of snake, and of other metalloproteinases of human origin which have been put in relation with various pathologies in man, including tumoral growth and metastatization, aterosclerosis, multiple sclerosis, Alzheimer's disease, osteoporosis, hypertension, rheumatoid arthritis and other inflammatory diseases. Object of the present invention is also the procedure for the production of diethylester of (1)-phosphotryptophan, as an initial product necessary to synthesize all compounds mentioned above.
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- Small organic molecule regulators of cell proliferation
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
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- Mediators of hedgehog signaling pathways, compositions and uses related thereto
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The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
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- Thiazolidinone compounds and composition for angina pectoris comprising the compounds as an active ingredient
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A thiazolidinone compound represented by general formula (I) or a pharmacoligically acceptable salt thereof, STR1 wherein W represents sulfur or oxygen and X represents --N(R1)--, or alternatively X represents sulfur or oxygen and W represents --N(R1)--, and R1 represents hydrogen, alkyl or substituted alkyl; R2 and R3 are the same or different from each other, and each represents hydrogen, alkyl, substituted alkyl, aryl, or 5- or 6-membered heteroaryl; R4 represents hydrogen, alkyl or substituted C1 -C4 alkyl; R5 represents substituted cycloalkyl which may contain nitrogen, provided the substituents include --B--ONO2 (wherein B represents a single bond or alkylene) as the indispensable member and alkyl groups as optional members; and A represents a single bond or alkylene, has an excellent anti-anginal effect and thus is useful as an angina pectoris remedy or preventive.
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- Process for the manufacture of brofaromine and analogs thereof
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A process for the manufacture of brofaromine and analogues thereof by reaction of a trisubstitued phosphonium methyl dihydroquinone compound with a 1-(substituted carbonyl)-4-(substituted carbonyl)-piperidine with subsequent cyclization and hydrolysis of the remaining carbonyl substituent. The resulting prmary compound can be further interconverted between free and salt forms or between different salt forms as desired.
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- Brain-specific drug delivery
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The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are: (a) compounds of the formula wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine pyridinium salt redox carrier, with the proviso that when [DHC] is STR1 wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH2 or OH function group to the carbonyl function of [DHC], then [D] must be other than a sympathetic stimulant, steroid sex hormone or long chain alkanol; and (b) non-toxic pharmaceutically acceptable salts of compounds of formula (I) wherein [D] is a centrally acting drug species and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine pyridinium salt redox carrier. The corresponding ionic pyridinium salt type drug/carrier entitles [D--QC]+ X- are also disclosed.
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- Brain-specific drug delivery
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The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are: (a) compounds of the formula wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine pyridinium salt redox carrier, with the proviso that when [DHC] is STR1 wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH2 or OH functional group to the carbonyl function of [DHC], then [D] must be other than a sympathetic stimulant, steroid sex hormone or long chain alkanol; and (b) non-toxic pharmaceutically acceptable salts of compounds of formula (I) wherein [D] is a centrally acting drug species and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine pyridinium salt redox carrier. The corresponding ionic pyridinium salt type drug/carrier entities [D-QC]+ Y- are also disclosed.
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- Benzophenone glycinamide derivatives
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This invention is directed toward pharmacologically active compounds of the formula STR1 wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula STR2 in which Ra represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C--Rb wherein Rb represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R1 represents a hydrogen atom or a lower alkyl group; R2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R3 represents a phenyl, halophenyl or 2-pyridyl group And acid addition salts thereof. Also provided are methods for their preparation and intermediates thereof. These compounds exhibit activity as anticonvulsants, muscle relaxants and sedatives.
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