2-[[tert-butyl(dimethyl)silyl]oxy]ethyl trifluoromethanesulfonate -Drug Synthesis Database

【结构式】

【分子编号】20297

【品名】2-[[tert-butyl(dimethyl)silyl]oxy]ethyl trifluoromethanesulfonate

【CA登记号】

【分子式】C₉H₁₉F₃O₄SSi

【分子量】308.3941696

【元素组成】C 35.05% H 6.21% F 18.48% O 20.75% S 10.4% Si 9.11%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号：(II)

Alkylation of rapamycin (I) with 2-(tert-butyldimethylsilyloxy)ethyl triflate (II) by means of 2,6-lutidine in hot toluene gives the silylated target compound (III), which is deprotected by means of 1N HCl in methanol.

参考文献中间体

合成目标

【1】 Castañer, J.; Sorbera, L.A.; Leeson, P.A.; SDZ-RAD. Drugs Fut 1999, 24, 1, 22.
【2】 Cottens, S.; Sedrani, R. (Novartis AG; Novartis Deutschland GmbH); O-Alkylated rapamycin derivs. and their use, particularly as immunosuppressants. EP 0663916; EP 0867438; JP 1996502266; JP 1999240884; US 5665772; WO 9409010 .

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	20296	(1R,9S,12S,15R,18R,19R,21R,23S,30S,32S,35R)-1,18-dihydroxy-12-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0(4,9)]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone	53123-88-9	C₅₁H₇₉NO₁₃	详情	详情
(II)	20297	2-[[tert-butyl(dimethyl)silyl]oxy]ethyl trifluoromethanesulfonate		C₉H₁₉F₃O₄SSi	详情	详情
(III)	20298	(1R,9S,12S,15R,18R,19R,21R,23S,30S,32S,35R)-12-[(1R)-2-[(1S,3R,4R)-4-(2-[[tert-butyl(dimethyl)silyl]oxy]ethoxy)-3-methoxycyclohexyl]-1-methylethyl]-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0(4,9)]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone		C₅₉H₉₇NO₁₄Si	详情	详情

Extended Information