- PROCESS FOR THE PREPARATION OF N(5)-ETHYLGLUTAMINE
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Disclosed relates to a process for preparing N (5)- ethylglutamines economically without a specific purification process via a simplified and safe process, in which glutamic acid derivatives, represented by formula 1, protected by phthaloyl groups react with ethylamine to cause an amidation and a deprotection reaction in turn under the same reaction condition, thus preparing N (5) -ethylglutamines .
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Page/Page column 13-15
(2008/06/13)
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- Inhibitors of caspases
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The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compoun
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- An efficient stereoselective synthesis of [3S(1S,9S)]-3-[[[9- (benzoylamino)octahydro-6,10-dioxo-6H-pyridazino-(1,2-a)(1,2)-diazepin-1- yl]-carbonyl]amino]-4-oxobutanoic acid, an interleukin converting enzyme (ICE) inhibitor
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The title compound 1 is a potent interleukin-1β-converting enzyme (ICE) inhibitor. Recently, an efficient chiral synthesis of compound 1 has been accomplished in our labs. The overall yield of this 18-step stereoselective synthesis was 9.8%.
- Chen,Goel,Hyun,Magano,Rubin
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p. 1587 - 1592
(2007/10/03)
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- SUBSTITUTED AZEPINONE DUAL INHIBITORS OF ANGIOTENSIN CONVERTING ENZYME AND NEUTRAL EXDOPEPTIDASE
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Compounds of the formula STR1 are disclosed as possessing inhibitory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.
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- COMPOUNDS CONTAINING A FUSED BICYCLE RING AND PROCESSES THEREFOR
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Compounds of the formula STR1 wherein X is O or S--(O) t ; n is one or two; m is zero or one; Y is CH 2, O, or S--(O) t provided that Y is O or S--(O) t only when m is one; and A is STR2 are dual inhibitors of NEP and ACE. Compounds wherein A is STR3 are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.
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- Peptidomimetic synthesis: Utilization of N-acyliminium ion cyclization chemistry in the generation of 7,6- and 7,5-fused bicyclic lactams
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A method for the stereoselective generation of 7,6- and 7,5-fused bicyclic lactams of type 1 has been developed. The key step involves intramolecular N-acyliminium ion cyclization of N-acyl enamine 2 to generate the core bicyclic framework. Lactams of typ
- Robl, Jeffrey A.
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p. 393 - 396
(2007/10/02)
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- Pyridazo[1,2-a][1,2]diazepines
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Novel compounds of the formula STR1 wherein B represents a methylene, ethylene or vinylene group, R1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylaminoalkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula STR2 R3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R4 and R5 each represent a hydrogen atom or R4 and R5 together represent an oxo group, R6 and R7 each represent a hydrogen atom or an alkyl or aralkyl group or R6 and R7 together with the nitrogen atom to which they are attached represent a 5-membered or 6-membered heteromonocyclic ring which may contain a further nitrogen atom or an oxygen or sulphur atom, and n stands for zero, 1 or 2, and pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations.
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