Benznidazole Synthetic Routes

CAT#: 329662 | Name: Benznidazole | CAS#

Description:

Benznidazole is an antiparasitic medication used in the treatment of Chagas disease. While it is highly effective in early disease this decreases in those who have long term infection. It is the first line treatment given its moderate side effects compared to nifurtimox. It is taken by mouth. Benznidazole is a nitroimidazole antiparasitic with good activity against acute infection with Trypanosoma cruzi, commonly referred to as Chagas disease. Like other nitroimidazoles, benznidazole's main mechanism of action is to generate radical species which can damage the parasite's DNA or cellular machinery. The mechanism by which nitroimidazoles do this seems to depend on whether or not oxygen is present. This is particularly relevant in the case of Trypanosoma species, which are considered facultative anaerobes.

Synthetic Routes

Benznidazole - Synthetic Route 1

Synthetic Description

Reference: Gandolfi Donadio, Lucia; Galetti, Mariana; Checura, Cintia C.; Santos, Marina; Comin, M. Julieta. A method for preparation of 2-nitroimidazoles and their intermediates. AR 97991. (Assignee Consejo Nacional de Investigaciones, Argent.; Instituto Nacional de Tecnologia Industrial (INTI))

Synthetic Reference

Gandolfi Donadio, Lucia; Galetti, Mariana; Checura, Cintia C.; Santos, Marina; Comin, M. Julieta. A method for preparation of 2-nitroimidazoles and their intermediates. AR 97991. (Assignee Consejo Nacional de Investigaciones, Argent.; Instituto Nacional de Tecnologia Industrial (INTI))

Benznidazole - Synthetic Route 2

Synthetic Description

Reference: Handal Vega, Erlinda; Arias Rivas, Carmen Elena; Cuchilla de Merlos, Ana Karina. Process for the solvent-free, catalyst-free microwave-assisted manufacture of the anti-Chagas N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide by solid phase amidation of N-benzyl-2-hydroxyacetamide with 2-nitro-1H-imidazole. WO 2015076760. (Assignee Ministerio de Educacion, El Salvador)

Synthetic Reference

Handal Vega, Erlinda; Arias Rivas, Carmen Elena; Cuchilla de Merlos, Ana Karina. Process for the solvent-free, catalyst-free microwave-assisted manufacture of the anti-Chagas N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide by solid phase amidation of N-benzyl-2-hydroxyacetamide with 2-nitro-1H-imidazole. WO 2015076760. (Assignee Ministerio de Educacion, El Salvador)

Benznidazole - Synthetic Route 3

Synthetic Description

Reference: Watson, Lynsey. Making benznidazole. WO 2017205622. (Assignee Savant Neglected Diseases, LLC, USA)

Synthetic Reference

Watson, Lynsey. Making benznidazole. WO 2017205622. (Assignee Savant Neglected Diseases, LLC, USA)

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