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US 10,519,104 B2Granted
Safe and efficient process for the preparation of carmustine
AssigneeNerPharMa S.r.l.
InventorsAttilio Tomasi, Ilaria Candiani, Francesco Corcella, Francesco Saverio Caldarelli
Life of this patent
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Abstract
Carmustine may be safely and efficiently produced by reacting 2-chloroethylamine hydrochloride and 1,1′-carbonyldiimidazole to afford 1,3-bis(2-chloroethyl)-1-urea, followed by nitrosation to give the final product.
Claims12
A process for the preparation of 1,3-bis(2-chloroethyl)-1-urea, which comprises:
- (a) reacting 2-chloroethylamine hydrochloride with carbonyldiimidazole in an aqueous medium in the absence of a base, to obtain N-(2-chloroethyl)-1H-imidazole-1-carboxamide of formula 3:
- and
- (b) reacting said N-(2-chloroethyl)-1H-imidazole-1-carboxamide with 2-chloroethylamine hydrochloride in an organic solvent or in an aqueous medium, to obtain 1,3-bis(2-chloroethyl)-1-urea.
A process for the preparation of 1,3-bis(2-chloroethyl)-1-nitrosourea, which comprises:
- (a) reacting 2-chloroethylamine hydrochloride with carbonyldiimidazole in an aqueous medium in the absence of a base, to obtain N-(2-chloroethyl)-1H-imidazole-1-carboxamide of formula 3:
- (b) reacting said N-(2-chloroethyl)-1H-imidazole-1-carboxamide with 2-chloroethylamine hydrochloride in an organic solvent or in an aqueous medium, to obtain 1,3-bis(2-chloroethyl)-1-urea;
- and
- (c) nitrosation of 1,3-bis(2-chloroethyl)-1-urea to obtain 1,3-bis(2-chloroethyl)-1-nitrosourea.
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