Table 1.

Preparation of epidithiodiketopiperazines from 3,6-diketopiperazines (DKPs).^[a]

Entry	Substrate	Product[b]	Overall yield (%)[c]
1	3	13	40
2	4	14	63
3	5	15	70
4	6	16	69
5	7	17	65
6	8	18	45
7	9	18	47
8	10	19	65
9	11	20	68
10	12	21	55[d]

^[a]Reactions were performed on 100 mg scale of DKP.

^[b]Racemic mixture unless otherwise stated.

^[c]Isolated yield after flash column chromatography.

^[d]ca. 1.4:1 dr.