反应 #470434

ord-360108300bf6452d9f8e4c75660e8a46

反应方程式

CCOC(=O)CCCCn1cc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc2n1
compound 0116-3
CCOC(=O)CCCCn1cc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc2n1
Ethyl 5-(4-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)-2H-indazol-2-yl)pentanoate
CCOC(=O)CCCCn1ncc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc21
compound 0115-3
CCOC(=O)CCCCn1ncc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc21
ethyl 5-(4-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)-1H-indazol-1-yl)pentanoate
CCOC(=O)CCCCCCBr
ethyl 7-bromoheptanoate
O=C([O-])[O-].[K+].[K+]
potassium carbonate
CCOC(=O)CCCCCCn1ncc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc21
title compound 0115-5
收率 27.0%
CCOC(=O)CCCCCCn1ncc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc21
ethyl 7-(4-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)-1H-indazol-1-yl)heptanoate
收率 27.0%
CCOC(=O)CCCCCCn1cc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc2n1
0116-5
收率 16.0%
CCOC(=O)CCCCCCn1cc2c(-c3nc(N4CCOCC4)c4sc(CN5CCN(S(C)(=O)=O)CC5)cc4n3)cccc2n1
Ethyl 7-(4-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)-2H-indazol-2-yl)heptanoate
收率 16.0%

反应条件

详细条件
See reaction.notes.procedure_details.

实验过程

The title compound 0115-5 (110 mg, 27%) and 0116-5 (60 mg, 16%) were prepared from 0114 (280 mg, 0.55 mmol) , ethyl 7-bromoheptanoate (133 mg, 0.65 mmol) and potassium carbonate (152 mg, 1.10 mmol) in acetonitrile (25 mL) using a procedure similar to that described for compound 0115-3 and compound 0116-3 (Example 1):

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08367663B2uspto-grants-2013_02