2(R)-(4-Methoxybenzyl)-3-(morpholinocarbonyl)propionic acid → (2S, 4S, 5S)-5-{N-[2(R)-(4-Methoxybenzyl)-3-(morpholinocarbonyl)propionyl]-3-(4-thiazolyl)-L-alanyl}amino-6-cyclohexyl-4-hydroxy-2-isopropyl-N-methylhexanamid

Participants

Reaction Steps

The procedure described in Example 1(b) was repeated, but using 200 mg (0.37 mmole) of (2S, 4S, 5S)-5-[N-(t-butoxycarbonyl)-3-(4-thiazolyl)-L-alanyl]amino-6-cyclohexyl-4-hydroxy-2-isopropyl-N-methylhexanamide [prepared as described in Example 1(a)] and 137 mg (0.45 mmole) of 2(R)-(4-methoxybenzyl)-3-(morpholinocarbonyl)propionic acid, to afford 188 mg (yield 70%) of the title compound as white crystals, melting at 128°-130° C.

Provenance & Evidence