Author: Schwartz, Theresa M. ; Lipton, Michael F. ; Mauragis, Michael A. ; Palmer, John R. ; Bundy, Gordon L. ; Zimmerman, David C. ; Veley, Michael F. ; Dobrowolski, Paul J. ; Banitt, Lee S.

A review.The pyrrolopyrimidines have been under study for several years at Pharmacia Corporation for a variety of potential therapeutic applications.This class of compound is typified by PNU-142731A and contains a tricyclic, generally fully aromatic nucleus, to which are appended two pyrrolidine moieties and a heterocycle-containing side chain.The process development aspects of the synthesis of four candidates in the series, and the application of lessons learned as the clin. program continued to evolve are presented.

01 Mar 2001·ORGANIC PROCESS RESEARCH & DEVELOPMENT

Synthesis of 2,4-Di-1-pyrrolidinyl-9H-pyrimido[4,5-b]indoles, Including Antiasthma Clinical Candidate PNU-142731A

Author: Zimmermann, David C. ; Schwartz, Theresa M. ; Banitt, Lee S. ; Veley, Michael F. ; Daugs, Edward D. ; Clouse, Robert C. ; Bundy, Gordon L. ; Palmer, John R. ; Appell, Robert B. ; Dobrowolski, Paul J. ; Lipton, Michael F. ; Mauragis, Michael A.

Two syntheses are described for 1-[(2,4-di-1-pyrrolidinyl-9H-pyrimido[4,5-b]indol-9-yl)acetyl]pyrrolidine hydrochloride (PNU-142731A), a clin. candidate in the asthma area.The route involving the initial regioselective addition of glycine Et ester to com. available 2,4,6-trichloropyrimidine is particularly well-suited for large-scale operation, as it is short, proceeds in good yield, is operationally straightforward, and requires no chromatog. purification of intermediates.

01 Dec 2000·Current opinion in investigational drugs (London, England : 2000)

Review

Author: Dent, G

Pharmacia is developing PNU-142731A, a potential lead compound as a treatment for asthma [294718]. It is in phase I clinical trials. PNU-142731A is a potent inhibitor of eosinophilic lung inflammation in rodents, and shows a good bioavailability profile in animals; the mechanism of action is being investigated. Unlike the original compound PNU-104067F, PNU-142731A does not give rise to gall bladder toxicity [295987], [298023].

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	-	Pfizer Inc.	-
Rhinitis, Allergic, Seasonal	Phase 2	-	Pfizer Inc.	-

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