- Benzo-fused lactams
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Compounds of the formula STR1 wherein A is STR2 are useful as ACE and NEP inhibitors and those wherein A is STR3 are useful as ACE inhibitors. Methods of preparation and intermediates are also disclosed.
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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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- TRANSITION METAL COMPLEXES - A NEW CLASS OF CATALYSTS OF INTERFACIAL ALKYLATION FOR THE ASYMMETRICAL SYNTHESIS OF α-AMINO ACIDS
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A new class of catalysts of interfacial asymmetrical alkylation is suggested for the synthesis of α-amino acids - positively charged complexes of the transition metals Cu(II), Ni(II), and Pd(II).These complexes consist of several fragments, by variation of which the structure of the catalysts can readily be modified.The complexes are chiral on account of (S)proline derivatives contained in them as one of the fragments.The catalyst complexes (C) were used in alkylation of amino acid fragments of Ni(II) complexes of the Schiff base of glycine with N-(2-pyridinecarbonyl)-o-aminobenzophenone (Ni-PBP-Gly) and the Schiff base of alanine with N-(2-pyridinecarbonyl)-o-aminobenzaldehyde (Ni-PBA-Ala) under interfacial conditions.After decomposition of alkylated complexes, phenylalanine and α-methyl-phenylalanine were isolated with yields of 33-87percent and optical purity (o. p.) from 3 to 21percent, depending on the C used.
- Belokon', Yu. N.,Maleev, V. I.,Videnskaya, S. O.,Saporovskaya, M. B.,Tsyryapkin, V. A.,Belikov, V. M.
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p. 110 - 118
(2007/10/02)
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- SYNTHESIS OF AMINO ACIDS. ALKYLATION OF ALDIMINE AND KETIMINE DERIVATIVES OF GLYCINE ETHYL ESTER UNDER VARIOUS PHASE-TRANSFER CONDITIONS
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The Schiff base derived from glycine ethyl ester and p-chlorobenzaldehyde can be alkylated by the ion-pair extraction method as well as under catalytic liquid-liquid or solid-liquid phase-transfer conditions.This imine is compared with the corresponding benzophenone Schiff base.
- Ghosez, Leon,Antoine, Jean-Pierre,Deffense, Etienne,Navarro, Mirtha,Libert, Valery,et al.
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p. 4255 - 4258
(2007/10/02)
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