Claims
- 1. A process for preparing: ##STR21## and its pharmaceutically acceptable salts and lower alkyl, aryl and aralkyl esters which comprises the steps of: treating: ##STR22## with NH.sub.2 R to form: ##STR23## followed by acetylating to form: ##STR24## followed by reducing to form: ##STR25## followed by cyclizing and deblocking to form: ##STR26## followed by alcoholysis with R.sup.1 OH to form: ##STR27## followed by cyclizing and deblocking to form: ##STR28## followed by treating with
- (R.sup.3 O.sub.2 CCH.sub.2 CO.sub.2).sub.2 Mg
- to form: ##STR29## followed by reacting with a carboxylic acid R.sup.8 COOH in the presence of a triorganophosphine and an activating agent therefor to yield: ##STR30## followed by deacylating and diazotization to provide: ##STR31## followed by cyclizing to form: ##STR32## followed by activating, treating with HSCH.sub.2 CH.sub.2 NHR.sup.4, and deprotecting wherein R.sup.1, R, R.sup.3 and ##STR33## are removable protecting groups.
- 2. The process of claim 1 wherein R.sup.1 OH is CH.sub.3 OH.
Parent Case Info
This is a continuation, of application Ser. No. 236,418, filed Feb. 20, 1981 now abandoned; which is a division of Ser. No. 112,022 filed Jan. 14, 1980, now U.S. Pat. No. 4,282,148.
US Referenced Citations (9)
Divisions (1)
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Date |
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112022 |
Jan 1980 |
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Continuations (1)
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236418 |
Feb 1981 |
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