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Synthesis of 2-amino-3,5-dihydro-7-(3-thienylmethyl)-[6-14C]-4H-pyrrolo[3,2-d]pyrimidin-4-one monohydrochloride ([14C]CI-1000)

✍ Scribed by James L. Hicks

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
290 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

2‐Amino‐3,5‐dihydro‐7‐(3‐thienylmethyl)‐[6‐^14^C]‐4H‐pyrrolo [3,2‐d]pyrimidin‐4‐one monohydrochloride ([^14^C]Cl‐1000), a potent purine nucleoside phosphorylase inhibitor, was made in six steps from potassium [^14^C]cyanide. A key step was the reduction of a nitro and a nitrile group with sodium hypophosphite and RaNi followed by cyclization of the resulting intermediate to form a pyrrolo[3,2‐d] pyrimidinone.

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