Table 1.

Residues R¹–R³ in intermediates 8 a–h, thioethers 9 a–d,f–h and thioester 9 e, and sulfoxides 10 a–d

Entry	R1	R2	R3	Yield[a] [%]
8 a	NH2	4‐Fluorobenzyl		85
8 b	NH2	4‐Phenylbenzyl		90
8 c	NH2	3,5‐Dimethoxybenzyl		76
8 d	NH2	2‐Pyridylmethyl		88
8 e	NH2	4‐Fluorbenzoyl		82
8 f	NH2	Piperidylethyl		87
8 g	NHCH3	Benzyl		89
8 h	CH3	4‐Fluorobenzyl		66
9 a	NH2	4‐Fluorobenzyl	3,4‐Difluorophenyl	35
9 b	NH2	4‐Phenylbenzyl	Ethoxy	38
9 c	NH2	3,5‐Dimethoxybenzyl	Ethoxy	52
9 d	NH2	2‐Pyridylmethyl	Ethoxy	30
9 e	NH2	4‐Fluorbenzoyl	Ethoxy	28
9 f	NH2	Piperidylethyl	Ethoxy	32
9 g	NHCH3	Benzyl	3,5‐Difluorobenzyl	8
9 h	CH3	4‐Fluorobenzyl	Ethoxy	84
10 a	NH2	4‐Fluorobenzyl	3,4‐Difluorobenzyl	30
10 b	NH2	4‐Phenylbenzyl	Ethoxy	88
10 c	NH2	3,5‐Dimethoxybenzyl	Ethoxy	18
10 d	CH3	4‐Fluorobenzyl	Ethoxy	25

[a] Isolated yield.