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. 2016 Jan 29;24(6):1241–1254. doi: 10.1016/j.bmc.2016.01.052

Table 2.

Coupling of P4 position and deprotection of t-butyl group

Entry Subst Conditionsa Product Entry Subst Conditionsa Product
1 4a graphic file with name fx2_lrg.gif 5a (38%) 9 4a graphic file with name fx10_lrg.gif 5i (69%)
2 4a graphic file with name fx3_lrg.gif 5b (79%) 10 4a graphic file with name fx11_lrg.gif 5j (55%)
3 4a graphic file with name fx4_lrg.gif 5c (37%) 11 4a graphic file with name fx12_lrg.gif 5k (29%)
4 4a graphic file with name fx5_lrg.gif 5d (43%) 12 4b graphic file with name fx13_lrg.gif 5l (26%)
5 4a graphic file with name fx6_lrg.gif 5e (80%) 13 4c graphic file with name fx14_lrg.gif 5m(91%)
6 4a graphic file with name fx7_lrg.gif 5f (7%) 14 4d graphic file with name fx15_lrg.gif 5n (19%)
7 4a graphic file with name fx8_lrg.gif 5g (23%) 15 4e graphic file with name fx16_lrg.gif 5o (48%)
8 4a graphic file with name fx9_lrg.gif 5h (29%)
a

Reagents and conditions: (1) conditions A, B or C, DIPEA, CH2Cl2, rt, (2) 50% TFA/CH2Cl2, rt. (A) HATU, HOAt, (B) DMT-MM, (C) Et3N, DMAP.