1226781-82-3

基本信息
奧格列汀雜質(zhì)10
奧格列汀中間體IV
MK-3102 中間體IV
5-BOC-2-(甲磺酰基)-2,4,5,6-四氫吡咯并[3,4-C]吡唑
2-(甲基磺?;?-2,6-二氫吡咯并[3,4-C]吡唑-5(4H)-甲酸叔丁酯
2-(甲基磺?;?-2,6-二氫吡咯并[3,4-C]吡唑-5(4H)-羧酸叔丁酯
2-(甲基磺酰基)-4,6-二氫吡咯并[3,4-C]吡唑-5(2H)-羧酸叔丁酯
2-(甲基磺?;?-4,6-二氫吡咯并[3,4-C]吡唑-5(2H)-甲酸叔丁酯
2-(甲基磺?;?-2,6-二氫吡咯并[3,4-C]吡唑-5(4H)-羧酸叔丁酯 奧格列汀中間體
MK-3103 Intermediate IV
Omarigliptin Impurity 10
Omarigliptin Intermediate 3
5-Boc-2-(methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole
tert-butyl 2-methanesulfonyl-2H,4H,5H,6H-pyrrolo[3,4-c]pyrazole-5-carboxylate
Pyrrolo[3,4-c]pyrazole, 2,4,5,6-tetrahydro-2-(methylsulfonyl)-, benzenesulfonate
tert-butyl 2-(Methylsulfonyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate
tert-butyl 2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazole-5(4H)-carboxylate
2-(Methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazole-5(4H)-carboxylic acid tert-butyl ester
物理化學(xué)性質(zhì)
常見問題列表

1280210-79-8

124-63-0
![2-(甲基磺?;?-2,6-二氫吡咯并[3,4-C]吡唑-5(4H)-羧酸叔丁酯](/CAS/20150408/GIF/1226781-82-3.gif)
1226781-82-3
將4,6-二氫吡咯并[3,4-c]吡唑-5(2H)-羧酸叔丁酯(3.5g,16.7mmol)溶解于四氫呋喃(35ml)中,冰浴冷卻至0℃。在氮氣保護下,緩慢加入氫化鈉(1.0g,60%分散于礦物油中,25.4mmol),保持0℃攪拌反應(yīng)30分鐘。隨后,逐滴加入甲基磺酰氯(2.9g,25.4mmol),繼續(xù)在0℃下攪拌反應(yīng)1小時。反應(yīng)完成后,緩慢加入水(10ml)淬滅反應(yīng),用乙酸乙酯(50ml×2)萃取。合并有機相,用無水硫酸鈉干燥,減壓濃縮。粗產(chǎn)物通過硅膠柱色譜法純化,洗脫劑為石油醚/乙酸乙酯(v/v=1:1),得到白色固體2-(甲基磺?;?-4,6-二氫吡咯并[3,4-c]吡唑-5(2H)-甲酸叔丁酯(2.1g,產(chǎn)率44%)。
參考文獻:
[1] Patent: EP3159344, 2017, A1. Location in patent: Paragraph 0096; 0132; 0133
[2] Patent: TW2017/8222, 2017, A. Location in patent: Page/Page column 54; 55
[3] Patent: TW2017/8223, 2017, A. Location in patent: Page/Page column 43
[4] Patent: WO2011/103256, 2011, A1. Location in patent: Page/Page column 55
[5] Patent: WO2011/146358, 2011, A1. Location in patent: Page/Page column 61