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. 2021 Mar 5;64(6):3299–3319. doi: 10.1021/acs.jmedchem.0c02191

Scheme 1. Reagents and General Conditions.

Scheme 1

(a) Ethyl bromoacetate, N,N-diisopropylethylamine (DIPEA), dimethylformamide (DMF) or benzylbromoacetate, Et3N, tetrahydrofuran (THF; when amine was used) and glycine ethyl ester hydrochloride, NaBH3CN, MeOH (when aldehyde or ketone was used); (b) (i) PivCl, DIPEA, dichloromethane (DCM); (ii) 2.5 N NaOH, MeOH or LiOH·H2O, MeOH/THF/H2O; (c) HATU, NMM, DM or EDCI, HOAt, DIPEA, DMF.