74654-91-4Relevant articles and documents
An improved large scale procedure for the preparation of N-Cbz amino acids
Pehere, Ashok D.,Abell, Andrew D.
scheme or table, p. 1493 - 1494 (2011/05/16)
A simple and scalable method for the preparation of N-Cbz protected amino acids is presented which uses a mixture of aqueous sodium carbonate and sodium bicarbonate to maintain the appropriate pH during the addition of benzyl chloroformate. The method has been extended to other N-protections and is amenable to large scale preparation of an intermediate toward Zofenopril, an ACE inhibitor.
1,1'-[DITHIOBIS(2-ALKYL-1-OXO-3,1-PROPANEDIYL)]-BIS[2,3-DIHYDRO-1H-INDOLE-2-CARBOXYLIC ACIDS AND DERIVATIVES
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, (2008/06/13)
Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,3-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 3-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: STR1 wherein: n is 1 or 0; R 1 is hydrogen, lower alkyl, aryl or aralkyl;R 2 is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl or aroyl; R. sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;R 4 is-SH, STR2 wherein L is O, NR 7 or S (where R 7 is hydrogen or lower alkyl); M is R 8, OR 8, SR 8, or NR 9 R 10 (where R 8 is hydrogen, lower alkyl, aryl, or aralkyl; and R 9 and R 10 are, independently, hydrogen, lower alkyl, or aryl); A is O, NR 13 or S;R 11 and R 12 are, independently, hydrogen, alkyl, aralkyl or aryl; R. sub. 13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3; R 20 is hydrogen or aryl; andR. sub. 21 is hydroxy or lower alkoxy;or pharmaceutically acceptable salts thereof.
N-(2-SUBSTITUTED-1-OXOALKYL)-2,3-DIHYDRO-1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVES
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, (2008/06/13)
Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substituted on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enz
