Use of vlb 3-(2-chloroethyl) carboxamide in treating neoplasms

Details Use of vlb 3-(2-chloroethyl) carboxamide in treating neoplasms Use of vlb 3-(2-chloroethyl) carboxamide in treating neoplasms

C - Chemistry, Metallurgy

07

D

260/237.3

C07D 519/04 (2006.01)

Patent

CA 1159055

Abstract A pharmaceutical formulation which comprises as an active ingredient (VLB or 4-desacetyl VLB) 3-(2- chloroethyl) carboxamide or a pharmaceutically-acceptable acid-addition salt thereof with a pharmaceutically- acceptable carrier therefor. Processes for preparing the active ingredient include (1) hydrolyzing the corresponding spirooxazolidinedione, (2) reacting the carboxazide with 2-chloroethylamine, and (3) reacting the 3-(2-hydroxyethyl)- carboxamide with a reagent which facilitates the replace- ment of a hydroxy function with chlorine and a source of chlorine. The process may include the optional steps of deacetylating, acetylating; and salifying the free base formed by the first-mentioned process of hydrolysis.

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