反应 #1881016

ord-101bae37fd2f4ebaaa02fc0ff0a9d8d2

反应方程式

COc1ccc(COC(=O)NC2CC=CCN(S(=O)(=O)c3ccc(OC)cc3)C2C(=O)OC(C)(C)C)cc1
1-(4-Methoxy-benzenesulfonyl)-3-(4-methoxybenzyloxy carbonyl-amino)-2,3,4,7-tetrahydro-1H-azepine-2-carboxylic acid tert-butyl ester
O=C(O)C(F)(F)F
Trifluoroacetic Acid
COc1ccc(S(=O)(=O)N2CC=CCC(N)C2C(=O)OC(C)(C)C)cc1
amine
COc1ccc(S(=O)(=O)N2CC=CCC(N)C2C(=O)OC(C)(C)C)cc1
3-Amino-1-(4-methoxy-benzenesulfonyl)-2,3,4,7-tetrahydro-1H-azepine-2-carboxylic acid tert-butyl ester

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他The solvents are evaporated

实验过程

1-(4-Methoxy-benzenesulfonyl)-3-(4-methoxybenzyloxy carbonyl-amino)-2,3,4,7-tetrahydro-1H-azepine-2-carboxylic acid tert-butyl ester (370 mg, 0.71 mMol) is dissolved in Dichloromethane (15 ml) containing 3% Trifluoroacetic Acid. The reaction is stirred for 1 h at room temperature. The solvents are evaporated and the remaining oil is co-evaporated twice with Toluene. Flash-chromatography Dichloromethane/Methanol (7:1) to afford the free amine: Cal. 546.6 found (M)+=547.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US07022690B2uspto-grants-2006_04