174767-74-9

Upstream product

• 182211-11-6 1-[((R)-1-Benzyloxycarbonylamino-2-phenyl-ethyl)-methoxy-phosphinoylmethyl]-cyclopentanecarboxylic acid tert-butyl ester 
• 174767-50-1 1-[((R)-1-Benzyloxycarbonylamino-2-phenyl-ethyl)-hydroxy-phosphinoylmethyl]-cyclopentanecarboxylic acid 
• 174767-53-4 (S)-2-({1-[((R)-1-Benzyloxycarbonylamino-2-phenyl-ethyl)-hydroxy-phosphinoylmethyl]-cyclopentanecarbonyl}-amino)-3-(1H-indol-3-yl)-propionic acid methyl ester 
• 174767-44-3 t-Butyl 1-[(trifluoromethanesulfonyl)oxy]methylcyclopentanecarboxylate 
• 137613-90-2 t-Butyl 1-(Hydroxymethyl)cyclopentanecarboxylate 
• 174850-07-8 methyl (1R)-1-<(benzyloxycarbonyl)amino>-2-phenylethyl phosphinate 
• 118636-74-1 ((R)-1-(((benzyloxy)carbonyl)amino)-2-phenylethyl)phosphinic acid 
• 7524-52-9 (S)-tryptophan methyl ester hydrochloride 

Relevant academic research and scientific papers

Design and synthesis of phosphinic acids that triply inhibit endothelin converting enzyme, angiotensin converting enzyme and neutral endopeptidase 24.11

We have synthesized a series of phosphinic acids as inhibitors of the metalloprotease endothelin converting enzyme (ECE). Potent ECE inhibitors 4g and 4o were identified. These compounds are members of a novel class of ECE inhibitors that are also potent inhibitors of angiotensin converting enzyme and neutral endopeptidase.

DERIVATIVES OF PHOSPHINIC ACID USEFUL AS ENDOTHELIN CONVERTING ENZYME INHIBITORS

Phosphinic acid derivatives of the structural formula STR1 or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R 1, R 2, R 3 and R. sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R 1 and R 2 form a cycloalkyl ring of 3-8 members and R 3 and R 4 are as defined; or R 3 and R 4 form a cycloalkyl ring of 3-7 members and R 1 and R 2 are as defined; or R 1 and R 2 together, and R 3 and R 4 together, each form a cycloalkyl ring;R 5 is--OR. sub.9 or--NHR 9, wherein R. sub.9 is hydrogen or alkyl;n is 0 or 1;A. sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A 1 and R 5 together form a radical of an α-aminoacyl derivative; andR. sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or--A 2--R. sub.7, wherein A 2 is a divalent α-aminoacyl radical, and R 7 is a substituent on the α-amino atom selected from H, R 8 OCO--, R. sub.8 SO 2--and R 8 NHCO--, wherein R 8 is aryl, arylmethyl or (C. sub.1-C 8)alkyl;are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R 3 and R 4 form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.