3543-73-5Relevant articles and documents
High-purity bendamustine hydrochloride intermediate preparation method
-
Paragraph 0036-0049, (2019/05/11)
The invention provides a high-purity bendamustine hydrochloride intermediate preparation method, wherein the intermediate is 5-amino-1-methyl-1H-2-benzimidazolebutyric acid ethyl ester, and the preparation method is characterized in that the mixed solvent of methanol and ethyl acetate is used. According to the present invention, with the preparation method, the impurities generated by the reduction reaction can be effectively reduced so as to obtain the high-purity intermediate and the final product bendamustine hydrochloride and reduce the difficulty in the industrial purification.
An efficient and facile synthesis of deuterium-labeled anticancer agent bendamustine hydrochloride
Liu, Baomin,Qin, Hui,Zhang, Yinsheng
, p. 869 - 874 (2018/06/04)
Bendamustine hydrochloride is an alkylating agent that was developed for the treatment of various human cancers. The stable isotope-labeled bendamustine was required to support clinic studies. An effective and operationally simple method for the synthesis of [D6] bendamustine hydrochloride was developed using DCl as a catalyst and D2O as a deuterium source. Under the present condition, regioselectively deuterated bendamustine hydrochloride with high deuterium incorporation is achieved.
Process for preparation of Bendamustine
-
, (2014/02/15)
The present invention relates to a method for preparation of alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5-oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4), b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro1H-benzimidazol-2-yl)butanoate (5), c) reduction of the product of step b) to alkyl 4-(5-amino-1-methyl-1H-benzimidazol-2-yl)butanoate (6), and d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7).
PROCESS FOR THE PREPARATION OF BENDAMUSTINE
-
, (2014/02/16)
The present invention relates to a method for preparation of alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: (a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5-oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4); (b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro1H-benzimidazol-2-yl)butanoate (5); (c) reduction of the product of step b) to alkyl 4-(5-amino-1-methyl-1H-benzimidazol-2-yl)butanoate (6), and (d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7)
Process for Preparation of Intermediates of Bendamustine
-
Paragraph 0023, (2013/12/04)
The present invention relates to a process for the preparation of 4-{5-{Bis-(2-hydroxyl-ethyl)-amino}-1-methyl-1H-Benzoimidazol-2yl}-butyric acid alkyl ester of formula IV, a key intermediate in the process for the preparation of Bendamustine HCl (I)
PROCESS FOR PREPARATION OF INTERMEDIATES OF BENDAMUSTINE
-
Page/Page column 4, (2012/02/02)
The present invention relates to a process for the preparation of 4-{5-{ Bis-(2-hydroxyl-ethyl)-amino}-1-methyl-1H-Benzoimidazol-2yl}-butyric acid alkyl ester of formula IV, a key intermediate in the process for the preparation of Bendamustine HCI (I)