- Completely Recyclable Monomers and Polycarbonate: Approach to Sustainable Polymers
-
It is of great significance to depolymerize used or waste polymers to recover the starting monomers suitable for repolymerization reactions that reform recycled materials no different from the virgin polymer. Herein, we report a novel recyclable plastic: degradable polycarbonate synthesized by dinuclear chromium-complex-mediated copolymerization of CO2 with 1-benzyloxycarbonyl-3,4-epoxy pyrrolidine, a meso-epoxide. Notably, the novel polycarbonate with more than 99 % carbonate linkages could be recycled back into the epoxide monomer in quantitative yield under mild reaction conditions. Remarkably, the copolymerization/depolymerization processes can be achieved by the ON/OFF reversible temperature switch, and recycled several times without any change in the epoxide monomer and copolymer. These characteristics accord well with the concept of perfectly sustainable polymers.
- Liu, Ye,Zhou, Hui,Guo, Jia-Zhi,Ren, Wei-Min,Lu, Xiao-Bing
-
-
Read Online
- Synthesis and diacylglycerol acyltransferase-1 inhibition of azabicyclo[3.1.0]hexane derivatives
-
We identified azabicyclo[3.1.0]hexane derivatives that are active diacylglycerol acyltransferase-1 (DGAT)-1 inhibitor. Among the azabicyclo[3.1.0]hexane series, compound 6b showed good in vitro activity toward human DGAT-1, selectivity toward DGAT-2, and
- Han, Seo-Jung,Lee, Gwi Bin,Kwak, Hyun Jung,Pagire, Suvarna H.,Kim, Ji Young,Pagire, Haushabhau S.,Park, Sung Bum,Chae, Chong Hak,Lee, Joo Yun,Kim, Ki Young,Rhee, Sang Dal,Kim, Hee Youn,Shin, Sun Hye,Bae, Myung Ae,Park, Mi-Jin,Kim, Dooseop,Lee, Duck Hyung,Ahn, Jin Hee
-
p. 1586 - 1593
(2015/07/15)
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- DEUTERATED HETEROCYCLIC COMPOUNDS AND THEIR USE AS IMAGING AGENTS
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The present invention relates to deuterated and optionally detectably labeled compounds of formula (I): R1-A-R2 and formula (V) and salts thereof, wherein Rl, R2, A, and X10-X19 have any of
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Page/Page column 37
(2016/01/22)
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- Tandem ring-closing metathesis/transfer hydrogenation: Practical chemoselective hydrogenation of alkenes
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An operationally simple chemoselective transfer hydrogenation of alkenes using ruthenium metathesis catalysts is presented. Of great practicality, the transfer hydrogenation reagents can be added directly to a metathesis reaction and effect hydrogenation of the product alkene in a single pot at ambient temperature without the need to seal the vessel to prevent hydrogen gas escape. The reduction is applicable to a range of alkenes and can be performed in the presence of aryl halides and benzyl groups, a notable weakness of Pd-catalyzed hydrogenations. Scope and mechanistic considerations are presented.
- Connolly, Timothy,Wang, Zhongyu,Walker, Michael A.,McDonald, Ivar M.,Peese, Kevin M.
-
supporting information
p. 4444 - 4447
(2015/01/09)
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- CELL PROLIFERATION INHIBITORS AND CONJUGATES THEREOF
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Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: [insert last structure from page 68 here] The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, optionally including a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.
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Page/Page column 256-257
(2014/10/04)
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- Enzymatic resolution of five membered heterocyclic bromohydrins
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The lipase catalyzed resolution of trans-3,4-tetrahydrofuran and pyrrolidine bromohydrins by acylation or hydrolysis of their acylated derivatives has been studied. For both heterocycles, the best enantioselectivity was obtained using Candida antarctica l
- Villar-Barro, Angela,Gotor, Vicente,Brieva, Rosario
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p. 694 - 698
(2013/07/11)
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- NOVEL COMPOUNDS
-
This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
- -
-
Paragraph 0394; 0395; 0396; 0397
(2013/06/26)
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- N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
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The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
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Page/Page column 148
(2012/08/08)
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- N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
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Page/Page column 190
(2012/08/08)
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- 3-HYDROXYPYRROLIDINE INHIBITORS OF 5?-METHYLTHIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE
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The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5?-methylthioadenosine phosphorylase or 5?-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5?-methylthioadenosine phosphorylase or 5?-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds
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Page/Page column 36
(2011/02/24)
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- TRIAZOLE COMPOUNDS AS KSP INHIBITORS
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The present invention provides triazole compounds of Formula I: as further described herein. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, and a method of treating a diso
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Page/Page column 14; 22
(2011/10/31)
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- PYRAZINYLPYRIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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The present invention provides a compound of Formula (I) and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.
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Page/Page column 71
(2011/04/14)
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- OXAZOLE AND THIAZOLE COMPOUNDS AS KSP INHIBITORS
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Disclosed are new substituted oxazole and thiazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof.
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Page/Page column 48
(2011/11/01)
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- HETEROARYL COMPOUNDS AS KINASE INHIBITORS
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The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor
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Page/Page column 72
(2011/04/14)
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- Design and synthesis of potent "sulfur-free" transition state analogue inhibitors of 5′-methylthioadenosine nucleosidase and 5′-methylthioadenosine phosphorylase
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5′-Methylthioadenosine/S-adenosylhomocysteine nucleosidase (MTAN) is a dual substrate bacterial enzyme involved in S-adenosylmethionine (SAM) related quorum sensing pathways that regulates virulence in many bacterial species. MTANs from many bacteria are directly involved in the quorum sensing mechanism by regulating the synthesis of autoinducer molecules that are used by bacterial communities to communicate. In humans, 5′-methylthioadenosine phosphorylase (MTAP) is involved in polyamine biosynthesis as well as in purine and SAM salvage pathways and thus has been identified as an anticancer target. Previously we have described the synthesis and biological activity of several aza-C-nucleoside mimics with a sulfur atom at the 5′ position that are potent E. coli MTAN and human MTAP inhibitors. Because of the possibility that the sulfur may affect bioavailability, we were interested in synthesizing "sulfur-free" analogues. Herein we describe the preparation of a series of "sulfur-free" transition state analogue inhibitors of E. coli MTAN and human MTAP that have low nano-to picomolar dissociation constants and are potentially novel bacterial anti-infective and anticancer drug candidates.
- Longshaw, Alistair I.,Adanitsch, Florian,Gutierrez, Jemy A.,Evans, Gary B.,Tyler, Peter C.,Schramm, Vern L.
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experimental part
p. 6730 - 6746
(2010/12/24)
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- Biocatalytic preparation of chiral 3,4-dihydroxypyrrolidines
-
Enzymatic acylations and alcoxycarbonylations of cis- and trans-3,4-dihydroxypyrrolidines and hydrolysis of their diacylated or dialcoxycarbonylated derivatives have been studied. High enantioselectivity is obtained using Candida antarctica lipase B as catalyst in the hydrolysis of the trans-diacetyl derivative, while for the desymmetrization of the cis-3,4-dihydroxypyrrolidines the best results are obtained in the acylation process catalyzed by C. antarctica lipase A.
- Rodríguez-Rodríguez, Jesús A.,Brieva, Rosario,Gotor, Vicente
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experimental part
p. 6789 - 6796
(2010/10/03)
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- Synthesis of iminodiacetaldehyde derivatives as building blocks for pharmacologically active agents
-
The preparation of iminodiacetaldehyde derivatives is reported via oxidative cleavage of 3,4-dihydroxypyrrolidines with sodium periodate. High yields of iminodiacetaldehydes are obtained starting from N-acyl-protected pyrrolidines, whereas the basic N-benzyl-protected derivative does not yield the expected dialdehyde. A cis-configured dihydroxypyrrolidine, prepared from 2,5-dihydropyrrole, reacts considerably faster with sodium periodate than the corresponding trans-configured derivatives which are obtained in three steps from (R,R)-tartaric acid. Georg Thieme Verlag Stuttgart.
- Fricke, Yvonne,Kopp, Nicole,Wuensch, Bernhard
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experimental part
p. 791 - 796
(2010/09/11)
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- NEW BRADYKININ B1 ANTAGONISTS
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The invention relates to compounds of formula (I) where in R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
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Page/Page column 199
(2010/04/03)
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- DISUBSTITUTED-AMINODIFLUOROSULFINIUM SALTS, PROCESS FOR PREPARING SAME AND METHOD OF USE AS DEOXOFLUORINATION REAGENTS
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The invention relates to disubstituted-aminodifluorosulfinium salts represented by the formula (I). Processes for preparing same and methods of use as deoxofluorinating reagent is also provided.
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Page/Page column 48-49
(2010/12/31)
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- Novel selective anti-androgens with a diphenylpentane skeleton
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We have proposed a multi-template approach for drug development, focusing on similar fold structures of proteins, and have effectively generated lead compounds for several drug targets. Modification of these polypharmacological lead compounds is then needed to generate target-selective compounds. In the work presented here, we aimed at separation of the anti-androgen activity and vitamin D activity of previously identified diphenylpentane lead compounds. Based on the determined X-ray crystal structures of androgen receptor and vitamin D receptor, bulky substituents were introduced at the t-butyl group in the lead compounds 2 and 3. As a result of this structural development, we obtained 16c, which exhibits more potent anti-androgen activity (IC 50: 0.13 μM) than clinically used anti-androgen bicalutamide (IC50: 0.67 μM) with 30-fold selectivity over vitamin D activity. This result indicates that lead compounds obtained via the multi-template approach can indeed be structurally modified to generate target-selective compounds.
- Maruyama, Keisuke,Noguchi-Yachide, Tomomi,Sugita, Kazuyuki,Hashimoto, Yuichi,Ishikawa, Minoru
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scheme or table
p. 6661 - 6666
(2010/12/19)
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- COMPOUNDS FOR TREATING DISORDERS MEDIATED BY METABOTROPIC GLUTAMATE RECEPTOR 5, AND METHODS OF USE THEREOF
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Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, psychiatric disorders, neuromuscular disorders, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds provided herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
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Page/Page column 148-149
(2010/11/03)
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- Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5
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A novel series of diaryl bicyclic azole-amines that are potent selective negative modulators of metabotropic glutamate receptor 5 (mGluR5) were identified through rational design. An initial hit compound 5a of modest potency (IC50 = 1.2 μM) was synthesized. Evaluation of structure-activity relationships (SAR) on the left-hand side of the molecule revealed a preference for a 2-substituted pyridine group linked directly to the central heterocycle. Variation of the central azolo-amine portion of the molecule revealed a preference for the [4,5-c]-oxazoloazepine scaffold, while right-hand side variants showed a preference for ortho- and meta-substituted benzene rings linked directly to the tertiary amine of the saturated heterocycle. These iterations led to the synthesis of 29b, a potent (IC50 = 16 nM) and selective negative modulator that showed good brain penetrance, high receptor occupancy, and a duration of action greater than 1 h in rat when administered intraperitoneally. Formal PK studies in rat and Rhesus monkey revealed a short half-life that was attributable to high first-pass clearance.
- Burdi, Douglas F.,Hunt, Rachel,Fan, Lei,Hu, Tao,Wang, Jun,Guo, Zihong,Huang, Zhiqiang,Wu, Chengde,Hardy, Larry,Detheux, Michel,Orsini, Michael A.,Quinton, Maria S.,Lew, Robert,Spear, Kerry
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supporting information; experimental part
p. 7107 - 7118
(2010/12/25)
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- Aminodifluorosulfinium salts: Selective fluorination reagents with enhanced thermal stability and ease of handling
-
Diethylaminodifluorosulfinium tetrafluoroborate (XtalFluor-E) and morpholinodifluorosulfinium tetrafluoroborate (XtalFluor-M) are crystalline fluorinating agents that are more easily handled and significantly more stable than Deoxo-Fluor, DAST, and their analogues. These reagents can be prepared in a safer and more cost-efficient manner by avoiding the laborious and hazardous distillation of dialkylaminosulfur trifluorides. Unlike DAST, Deoxo-Fluor, and Fluolead, XtalFluor reagents do not generate highly corrosive free-HF and therefore can be used in standard borosilicate vessels. When used in conjunction with promoters such as Et3N3HF, Et3N2HF, or DBU, XtalFluor reagents effectively convert alcohols to alkyl fluorides and carbonyls to gem-difluorides. These reagents are typically more selective than DAST and Deoxo-Fluor and exhibit superior performance by providing significantly less elimination side products.
- Lheureux, Alexandre,Beaulieu, Francis,Bennett, Christopher,Bill, David R.,Clayton, Simon,Laflamme, Franois,Mirmehrabi, Mahmoud,Tadayon, Sam,Tovell, David,Couturier, Michel
-
experimental part
p. 3401 - 3411
(2010/07/07)
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- PQS: A new platform for micellar catalysis. RCM reactions in water, with catalyst recycling
-
(Chemical Equation Presented) The first "designer" surfactant containing a covalently bound ruthenium catalyst is reported. This species dissolves freely in water, forming nanomicelles in which ring-closing metathesis reactions on water-insoluble dienic s
- Lipshutz, Bruce H.,Ghorai, Subir
-
supporting information; experimental part
p. 705 - 708
(2009/08/12)
-
- 5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE-DERIVATIVES AND THEIR USES AS ANTIBACTERIALS
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The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; Rsup
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Page/Page column 14
(2009/10/06)
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- Aminodifluorosulfinium Tetrafluoroborate salts as stable and crystalline deoxofluorinating reagents
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Aminodifluorosulfinium tetrafluoroborate salts were found to act as efficient deoxofluorinating reagents when promoted by an exogenous fluoride source and, In most cases, exhibited greater selectivity by providing less elimination byproduct as compared to DAST and DeoxoFluor. Aminodifluorosulfinium tetrafluoroborates are easy handled crystalline salts that show enhanced thermal stability over dialkylaminosulfur trifluorides, are storage-stable, and unlike DAST and Deoxo-Fluor do not react violently with water.
- Beaulieu, Francis,Beauregard, Louis-Philippe,Courchesne, Gabriel,Couturier, Michel,Laflamme, Francois,L'Heureux, Alexandre
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supporting information; experimental part
p. 5050 - 5053
(2009/12/28)
-
- 5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES
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The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; Rs
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Page/Page column 33-34
(2008/12/05)
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- AMINOPYRROLIDINE COMPOUND
-
Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.
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Page/Page column 74
(2009/01/24)
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- Synthesis of conformationally restricted acetylcholine analogues. Comparing lipase-mediated resolution with simulated moving bed chromatography of arylated β-hydroxy-pyrrolidines
-
The enantiodivergent synthesis of new, conformationally restricted acetylcholine analogues was accomplished using arylated endocyclic enecarbamates as key intermediates. Stereoselective hydroboration of the aryl enecarbamates provided the corresponding ar
- Barreto, Ricardo de L.,Carpes, Marcos J.S.,Santana, Cesar C.,Correia, Carlos R.D.
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p. 435 - 442
(2007/10/03)
-
- Synthesis of the 3-(3,4,5-trimethoxyphenyl)-pyrrolidine: A new conformationally constrained mescaline analogue
-
The total synthesis of the 3-(3,4,5-trimethoxyphenyl)-pyrrolidine, a new and conformationally constrained mescaline analogue, was accomplished in a concise and efficient manner. The synthetic route encompassed only 4 steps from the starting N-Cbz-3-pyrrol
- Barreto, Ricardo De L.,Nascimbem, Laura B. L. R.,Correia, Carlos Roque Duarte
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p. 2011 - 2018
(2008/02/05)
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- Chemoenzymatic synthesis of (3R,4S)- and (3S,4R)-3-methoxy-4-methylaminopyrrolidine
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An efficient and a convenient enantioselective synthesis of (3R,4S)-3-methoxy-4-methylaminopyrrolidine has been carried out by a lipase-mediated resolution protocol. This method describes the preparation of (±)-1-Cbz-cis-3-azido-4-hydroxypyrrolidine start
- Kamal, Ahmed,Shaik, Ahmad Ali,Sandbhor, Mahendra,Malik, M. Shaheer,Azeeza, Shaik
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p. 2876 - 2883
(2007/10/03)
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- 7-SUBSTITUTED IMIDAZO[4,5-C]PYRIDINE ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE RECEPTOR
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The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.
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Page/Page column 13; 19
(2008/06/13)
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- COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS
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The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula (I) are provided or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer, and osteolytic bone disorders.
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Page/Page column 124-125
(2008/06/13)
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- New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors
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Cyclohexylglycine amides of various fluorinated pyrrolidines and azetidines were prepared and tested for activity against dipeptidyl peptidase IV and in vivo in the KK mouse model of type 2 diabetes. The tetrafluoropyrrolidide, cis-3,4-difluoropyrrolidide and the fluorinated azetidides displayed unexpectedly strong activity.
- Hulin, Bernard,Cabral, Shawn,Lopaze, Michael G.,Van Volkenburg, Maria A.,Andrews, Kim M.,Parker, Janice C.
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p. 4770 - 4773
(2007/10/03)
-
- Therapeutic compounds
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The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.
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Page/Page column 12
(2008/06/13)
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- Chemoenzymatic synthesis of (3S,4S)- and (3R,4R)-3-methoxy-4- methylaminopyrrolidine
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Facile chemoenzymatic enantioselective synthesis of (3S,4S)-3-methoxy-4- methylaminopyrrolidine, a key intermediate for a new quinolone antitumor compound AG-7352 has been described. This methodology illustrates the preparation of 3-azido-1-benzyloxycarbo
- Kamal, Ahmed,Shaik, Ahmad Ali,Sandbhor, Mahendra,Malik, M. Shaheer,Kaga, Harumi
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p. 8057 - 8059
(2007/10/03)
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- Highly diastereoselective additions to polyhydroxylated pyrrolidine cyclic imines: Ready elaboration of aza-sugar scaffolds to create diverse carbohydrate-processing enzyme probes
-
Representative diastereomeric, erythritol and threitol polyhydroxylated pyrrolidine imine scaffolds have been rapidly elaborated to diversely functionalized aza-sugars through highly diastereoselective organometallic (RM) additions (R = Me, Et, allyl, hex
- Chapman, Timothy M.,Courtney, Steve,Hay, Phil,Davis, Benjamin G.
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p. 3397 - 3414
(2007/10/03)
-
- Novel cyclic sugar imines: carbohydrate mimics and easily elaborated scaffolds for aza-sugars.
-
[reaction: see text] Representative simple or polyhydroxylated, pyrrolidine (e.g, DRAM) or piperidine (e.g., DNJ) imines not only are potential carbohydrate-processing enzyme inhibitors that may be formed as regioisomeric variants but also are scaffolds that may be rapidly elaborated to diversely functionalized aza-sugars through highly diastereoselective organometallic additions.
- Davis, Benjamin G,Maughan, Michael A T,Chapman, Timothy M,Villard, Renaud,Courtney, Steve
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p. 103 - 106
(2007/10/03)
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- Olefin metathesis in non-degassed solvent using a recyclable, polymer supported alkylideneruthenium
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Polystyrene-supported ruthenium complex 8 is a robust procatalyst for olefin metathesis that can be used in non-degassed solvents and recycled without added stabilisers.
- Dowden,Savovic
-
-
- Generation of cyclopenta[c]piperidines and pyrrolo[3,4-c]piperidines-Potential substance P antagonists - From adducts of cyclic dienophiles and 5-chloro-6-methyl-3-phenyl-2H-1,4-oxazin-2-one
-
1,1,4,4-Tetrasubstituted cyclopenta[c]piperidines and the corresponding 4,4,7,7-pyrrolo[3,4-c]piperidines have been synthesised via cycloaddition of 5-chloro-6-methyl-3-phenyl-2H-1,4-oxazin-2-one with cyclopentene and 3-pyrroline derivatives, respectively, followed by reductive opening of the lactone-bridged adducts. The axial-equatorial conformational preferences of the substituents in these cis-fused bicyclic systems were opposite to those for the monocyclic piperidine analogues. The specific array of functional groups in the bicyclic aminoalcohols was used to accommodate, in stereocontrolled fashion, variable pharmacophoric groups that are of interest for substance P antagonist activity. (C) 2000 Elsevier Science Ltd.
- Wu, Xiujuan,Toppet, Suzanne,Compernolle, Frans,Hoornaert, Georges J.
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p. 6279 - 6290
(2007/10/03)
-
- Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds
-
A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylatio
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-
-
- Cephalosporin compounds and processes for preparing thereof
-
Quaternary ammoniocephalosporins of formula(I) wherein Q=CH or N, P=hydroxylated amine or hydroxylated heterocyclylamines including N-methyl-bis(2-hydroxyethyl)amine, rac-3,4-trans-dihydroxy-1-methylpyrrolidine, (3S, 4S)-3,4-dihydroxy-1-methylpyrrolidine,
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-
-
- Water-Soluble Renin Inhibitors: Design of a Subnanomolar Inhibitor with a Prolonged Duration of Action
-
Incorporation of nonreactive polar functionalities at the C- and N-termini of renin inhibitors led to the development of a subnanomolar compound (21) with millimolar solubility.This inhibitor demonstrated excellent efficacy and a long duration of action upon intravenous administration to monkeys.While activity was also observed intraduodenally, a comparison of the blood pressure responses indicated low bioavailability.Subsequent experiments in rats showed that, although the compound was absorbed from the gastrointrestinal tract, extensive liver extraction severely limited bioavailability.
- Rosenberg, Saul H.,Woods, Keith W.,Sham, Hing L.,Kleinert, Hollis D.,Martin, Donald L.,et al.
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p. 1962 - 1969
(2007/10/02)
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