反应详情

Compound 10 (Reaction Scheme 4) was obtained in three synthetic steps. Methyl 2-isocyanoacetate reacted with 4-fluorobenzaldehyde and KOH in MeOH for 7 h at room temperature to afford diastereoselectivity and quantitatively the crude potassium salt trans-ANP 20162. Potassium salt ANP 20162 was coupled with 4-methylpiperidine using the EDCI-HOBT method in dichloromethane to produce the oxazoline amide, LPO 26074 Oxazoline LPO 26074 then underwent ring opening using a HCl 37% solution in MeOH at 45° C. for 15 min to give Compound 10 in 7% yield after purification.

1. customto afford diastereoselectivity