Bedaquiline

CAT#: H314214

CAS#: 843663-66-1

Description: Bedaquiline, also known as TMC207 and R207910, is a diarylquinoline anti-tuberculosis drug, which was discovered by a team led by Koen Andries at Janssen Pharmaceutica. Bedaquiline blocks the proton pump for ATP synthase of mycobacteria. ATP production is required for cellular energy production and its loss leads to cell death, even in dormant or nonreplicating mycobacteria.It is the first member of a new class of drugs called the diarylquinolines. Bedaquiline is bactericidal.

img

Synthetic Routes

Bedaquiline - Synthetic Route 1

Bedaquiline route01

Synthetic reference

Saga, Yutaka; Motoki, Rie; Makino, Sae; Shimizu, Yohei; Kanai, Motomu; Shibasaki, Masakatsu. Catalytic Asymmetric Synthesis of R207910. Journal of the American Chemical Society. Volume 132. Issue 23. Pages 7905-7907. Journal. (2010).

Bedaquiline - Synthetic Route 2

Bedaquiline route02

Synthetic reference

Kong, De-Long; Huang, Ye; Ren, Lai-Yang; Feng, Wen-Hua. A highly efficient way to recycle inactive stereoisomers of Bedaquiline into two previous intermediates via base-catalyzed Csp3-Csp3 bond cleavage. Chinese Chemical Letters. Volume 26. Issue 6. Pages 790-792. Journal; Online Computer File. (2015).

Bedaquiline - Synthetic Route 3

Bedaquiline route03

Synthetic reference

Li, Jianqi; Liu, Yu; Bing, Shaochang; Wu, Xiabing; Zhou, Ainan; Huang, Lei; Jin, Renli; Wang, Jian; Jiang, Min; Wang, Lei. Method for preparing bedaquiline. Assignee China National Medicines Guorui Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Institute of Pharmaceutical Industry. CN 105085395. (2015).