Water → (7R)-7-[(2-aminoethyl)(methyl)amino]-14-cyclohexyl-N-{[methyl(2-oxoethyl)amino]sulfonyl}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxamide

Participants

Reaction Conditions

Reaction Steps

A solution of tert-butyl {2-[{(7R)-14-cyclohexyl-11-[({[(2,2-dimethoxyethyl)-(methyl)amino]sulfonyl}amino)carbonyl]-7,8-dihydro-6H-indolo[1,2-e][1,5]-benzoxazocin-7-yl}(methyl)amino]ethyl}carbamate (0.03 M) in DCM was treated with TFA (100 eq) and water (180 eq) at RT and the resulting mixture stirred vigorously for 3 h at 40° C. The volatiles were removed in vacuo and the residue diluted with Et2O and re-evaporated to drive off excess TFA. The product was used in the subsequent step without further purification. MS (ES+) m/z 582 (M+H)+; 600 (M+H2O+H)+.

Provenance & Evidence