1547229-17-3Relevant academic research and scientific papers
COMPOUND AND METHOD FOR MANUFACTURING THE SAME, AND METHOD FOR MANUFACTURING VORICONAZOLE
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Paragraph 0066, (2016/11/14)
PROBLEM TO BE SOLVED: To provide a method for manufacturing voriconazole, which is a therapeutic agent for severe or intractable deep mycosis such as aspergillosis, allowing easy manufacture without the need for the optical resolution. SOLUTION: A method for manufacturing voriconazole includes: obtaining a compound represented by the general formula (3) by using catalytic asymmetric cyanoacylation reaction; and reacting the compound with 1,2,4-triazole to convert it into voriconazole. [In the general formula (3), X is any of the divalent groups represented by the specified structural formulas.] COPYRIGHT: (C)2015,JPOandINPIT
An enantioselective synthesis of voriconazole
Tamura, Keiji,Furutachi, Makoto,Kumagai, Naoya,Shibasaki, Masakatsu
supporting information, p. 11396 - 11403 (2013/12/04)
A new seven-step sequence to access voriconazole, a clinically used antifungal agent, was developed. The initial catalytic asymmetric cyanosilylation is the key to constructing the consecutive tetra- and trisubstituted stereogenic centers. The fluoropyrimidine unit frequently triggered unexpected side reactions, but careful amendment of the reaction sequence allowed for the concise enantioselective synthesis.
