Table 3.

Final solvent optimization for MACOS preparation of sultam (4) sublibrary.

Entry	R2	X	Solvent	Time of run (min)	Conversion [%]	Yield [%][a]	Product (grams produced)
1	Me	4-Br	DMF	25	100	53	4i (R) (0.1)
2	Me	4-Br	DMA	25	100	52	4i (R) (0.1)
3	Me	4-Br	NMP	25	100	49	4i (R) (0.09)
4	Me	4-Br	DMSO	25	100	78	4i (R) (0.15)
5	Me	4-Br	DMSO	120	–	80	4i (R) (6.65)
6	Me	4-Br	DMSO	120	–	75	4i (S) (4.21)
7	Ph	4-Br	DMSO	120	–	73	4a (R) (2.07)
8	iBu	4-Br	DMSO	120	–	80	4c (R) (8.53)
9	iBu	4-Br	DMSO	120	–	93	4c (S) (9.48)
10	Bn	4-Br	DMSO	120	–	86	4d (R) (9.83)
11	Bn	4-Br	DMSO	120	–	85	4d (S) (10.1)
12	Me	6-F	DMSO	120	–	84	4j (R) (7.72)
13	Me	6-F	DMSO	120	–	84	4j (S) (7.5)
14	iBu	6-F	DMSO	120	–	92	4 f (R) (9.9)
15	iBu	6-F	DMSO	120	–	89	4 f (S) (9.5)
16	Bn	6-F	DMSO	120	–	79	4k (R) (8.4)
17	Bn	6-F	DMSO	120	–	87	4k (S) (10.57)
18	Me	4-F	DMSO	120	–	79	4l (R) (8.45)
19	Me	4-F	DMSO	120	–	76	4l (S) (7.1)
20	iBu	4-F	DMSO	120	–	91	4h (R) (10.37)
21	iBu	4-F	DMSO	120	–	96	4h (S) (10.89)
22	Bn	4-F	DMSO	120	–	72	4m (R) (6.05)
23	Bn	4-F	DMSO	120	–	72	4m (S) (7.55)

^[a]Yields of isolated product after column chromatography.