Tetrahedron Letters p. 563 - 566 (1996)
Update date:2022-09-26
Topics:
Weisz, Imre
Roboz, John
Bekesi, J. George
L-propyl-L-m-[bis(chloroethyl)amino]-phenylalanyl-L-norvaline ethyl ester hydrochloride, 4 (and its 3H and 14C doubly-labeled version) was synthesized starting with reacting unprotected L-m-sarcolysin, 1, with TFA-Pro-Cl in an acidic system to yield TFA-Pro-L-m-sarcolysin, 2, which was transformed to the TFA-tripeptide ethyl ester, 3. Selective aminolytic cleavage of the TFA group with butylamine in abs. ethanol, followed by neutralization with HCl gave 4.
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