METHOD OF SYNTHESIS OF 1-(2-CHLOROETHYL)-3-CYCLO-HEXYL-1-NITROSOUREA Russian patent published in 2002 - IPC

Abstract RU 2192413 C1

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to method of synthesis of 1-(2-chloroethyl)-3-cyclohexyl-1- nitrosourea known in pharmacy as antitumor preparation lomustine. By the proposed method lomustine is synthesized for some stages: by interaction of cyclohexylisocyanate with monoethanolamine in acetonitrile medium and feeding the reaction product directly to the next stage of reaction product treatment with thionyl chlioride in toluene medium in the presence of zinc chloride as catalyst; by interaction of synthesized chloroethyl derivative with sodium nitrite in 75-85% aqueous formic acid solution, the following treatment of isomers mixture formed with hydrochloric acid and crystallization of end product from mixture acetone/acetonitrile. Method ensures to increase the yield of end product of pharmacopoeia quality to 51.7%. EFFECT: improved method of synthesis, increased yield, simplified process. 1 ex

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RU 2 192 413 C1

Authors

Romanova O.B.

Sorokina I.K.

Krivtsova I.Ju.

Budanova L.I.

Gojzman M.S.

Granik V.G.

Dates

2002-11-10—Published

2001-03-12—Filed