With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3405-77-4,5-Methylisoxazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.
(2R,6S,13aS,14aR,16aS,Z)-ethyl 6-(5-methylisoxazole-3-carboxamido)-2-(4- nitrobenzoyloxy)-5,16-dioxo-l,2,3,5,6,7,8,9,10,l l,13a,14,14a,15, 16,16a- hexadecahydrocyclopropa[e]pyrrolo[l,2-a][l,4]diazacyclopentadecine-14a-carboxylate; To a solution of (2R,6S,13aS,14aR,16aS,Z)-14a-(ethoxycarbonyl)-2-(4-nitrobenzoyloxy)- 5,16-dioxo-l,2,3,5,6,7,8,9,10,l l,13a,14,14a,15,16,16a- hexadecahydrocyclopropa[e]pyrrolo[l,2-a][l,4]diazacyclopentadecin-6-aminium 4- methylbenzenesulfonate (9.95 g), 5-methylisoxazole-3-carboxylic acid (2.12 g), and NMP (30.0 g) at 5 ¡ãC was added diisopropylethylamine (6.5 g). Propanephosphonic acid anhydride (5.3 g) was charged as a solution in EtOAc (5.3 g) and NMP (10 mL) to the reaction mixture. The reaction was warmed to rt over 14 h. The reaction solution was diluted with 2-Me-THF (150 mL). The diluted reaction solution was washed with water (150 mL), a 1.0 M aqueous solution of H3PO4 (2 x 50 mL), water (50 mL), a 5percent aqueous solution of NaHC03 (50 mL), and then a 10percent aqueous solution of NaCl (2 x 50 mL). The organic solution was dried over MgS04, filtered, and then concentrated under reduced pressure, and then co-distilled with THF (200 mL). THF was added and the product-containing solution was filtered and evaporated to an oil (8.5 g, 93percent yield).
3405-77-4, The synthetic route of 3405-77-4 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; ABBOTT LABORATORIES; ENANTA PHARMACEUTICALS, INC.; CHEN, Hui-ju; MCDANIEL, Keith, F.; GREEN, Brian, E.; SHANLEY, Jason, P.; KRUGER, Albert, W.; GANDARILLA, Jorge; WELCH, Dennie, S.; CINK, Russell, D.; GAI, Yonghua; WANG, Guoqiang; OR, Yat, Sun; WO2011/156337; (2011); A2;,
Isoxazole – Wikipedia
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