Total synthesis of (8R)-3-(2-deoxy-. beta.-D-erythro-pentofuranosyl)-3, 6, 7, 8-tetrahydroimidazo [4, 5-d][1, 3] diazepin-8-ol (pentostatin), the potent inhibitor of …

…, SR Putt, HDH Showalter, DC Baker

文献索引：Chan; Putt; Showalter; Baker Journal of Organic Chemistry, 1982 , vol. 47, # 18 p. 3457 - 3464

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被引用次数: 58

摘要

A definitive synthesis for the potent adenosine deaminase inhibitor (8R)-3-(2-deoxy-P-~- erythro-pento-furanosyl)-3, 6, 7, 8-tetrahydroimidazo [4, 5-d][1, 3] diazepin-8-01 (l) lS and ita 8s isomer 13 is described, beginning with imidazole precursors. Construction of the heterocyclic portion 11 was accomplished by ring closure of the diamine 10 using triethyl orthoformate; 10 was prepared in eight steps from 4-methyl-5-nitroimidazole (4). ...