MX-1013, Z-VD-fmk, CV-1013

Chemical Name: N-(Benzyloxycarbonyl)-L-valyl-DL-aspartyl-fluoromethane
CAS No. 223568-55-6 ((S)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Cytovia (Originator), Maxim (Licensee)
合成路线:2-Fluoroethanol (I) was oxidized under Swern conditions to afford 2-fluoroacetaldehyde (II),which was condensed with tert-butyl 3-nitropropionate (III),yielding the hydroxy ester (IV).Hydrogenation of the nitro group of (IV) over Raney nickel produced amine (V).Subsequent coupling of N-carbobenzoxy-L-valine (VI) with amine (V) in the presence of EDC and HOBt furnished amide (VII).The hydroxyl group of (VII) was then oxidized to the corresponding ketone (VIII) by using Dess-Martin periodinane.Finally,the tert-butyl ester was cleaved by treatment with trifluoroacetic acid.