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US 2019/0169116 A1Published application
Process for preparation of carmustine
AssigneeIntas Pharmaceuticals Ltd.
InventorsGobind Singh KAPKOTI, Nirmal KUMAR, Mettilda LOURDUSAMY, Ioan-Iosif RADU, Aakash Maheshkumar SHAH, Hitesh Manubhai MAKWANA, Mohamed Zuber Abdulhaq SHAIKH, Yogesh Naranbhai VAGHASIYA
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Abstract
The present invention relates to an improved process for preparation of carmustine (I). The present invention also relates to preparation of 1,3-bis(2-chloroethyl)urea (II) an intermediate used in preparation of carmustine.
Claims11
A process for preparation of carmustine (I)
- comprising a step of:
- a) converting 2-chloroethylamine (III) to 1,3-bis(2-chloroethyl)urea (II)
- in absence of phosgene.
A process for preparation of carmustine (I)
- comprising steps of:
- a) converting 2-chloroethylamine (III) to 1,3-bis(2-chloroethyl)urea (II)
- in absence of phosgene.
- b) converting urea of formula (II) to carmustine (I).
1 more element
A process for preparation of carmustine (I) comprising steps of:
- a) reacting 2-chloroethyl amine (III) or its salt with a reagent selected from 1,1′-carbonyldiimidazole, triphosgene and phenyl chloroformate in presence of base to obtain 1,3-bis (2-chloroethyl) urea (II);
- b) reacting 1,3-bis(2-chloroethyl)urea with nitrosating reagent in presence of solvent to obtain carmustine;
- wherein step (a) is carried out in absence of phosgene.
Dependencies are inferred from the claim text.