Synthesis of 2,4-Di-1-pyrrolidinyl-9H-pyrimido[4,5-b]indoles, Including Antiasthma Clinical Candidate PNU-142731A
Organic Process Research & Development2001Vol. 5(2), pp. 144–151
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Gordon L. Bundy, Lee S. Banitt, Paul J. Dobrowolski, John R. Palmer, Theresa Schwartz, David C. Zimmermann, Michael F. Lipton, M. A. Mauragis, Michael F. Veley, Robert B. Appell, Robert C. Clouse, Edward D. Daugs
Abstract
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 clinical candidate in the asthma area. The route involving the initial regioselective addition of glycine ethyl ester to commercially 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 chromatographic purification of intermediates.
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