6296-89-5Relevant articles and documents
A greener approach for the large-scale synthesis of 1,4,5-trisubstituted pyrazole, AZD8329
Rangappa, Paramashivappa,Ghosh, Avipsa,Chitrapadi, Smitha,Kantikar, Gajanan,Ch, Vinod Kumar,Sythana, Sureshkumar,Manjunath, Sulur G.,Nambiar, Sudhir,Sridhran
, p. 947 - 951 (2014/10/15)
The development of a convenient, safe and scalable process for AZD8329 manufacturing is reported here. Synthesis was achieved in a two-step telescopic process with an excellent overall yield of 75%. In the first step enamine (6) was synthesized with 90% yield through three chemical transformations. In the next step AZD8329 was synthesized from the reactions of 6 and 4-hydrazinobenzoic acid hydrochloride 7 through two chemical transformations. The process is very efficient and economical, and AZD8329 was manufactured in multikilogram scale. A greener approach is demonstrated through usage of a minimum number of solvents and energy and with process mass intensity (PMI) 60 in the manufacturing process.
PYRAZOLE DERIVATIVES AS 11-BETA-HSD1 INHIBITORS
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Page/Page column 155-156, (2008/12/08)
A compound of formula (I): and pharmaceutically -acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.