Trimethyl phosphite → HCID 86618181, compound

Participants

Reaction Steps

The title compound was prepared from 1-bromo-1-[3-(2-bromo-2-methylpropanoyl)-6-methoxy-1H-indazol-1-yl]-3,3-dimethylbutan-2-one from Step A above and trimethyl phosphite using the method in Method I Step B of Example 1. It was purified by RP-HPLC using 10-80% MeCN gradient without TFA. 1H NMR (CDCl3, 500 MHz) δ 7.68 (d, 8.9 Hz, 1H), 6.865 (dd, 2.1 & 8.9 Hz, 1H), 6.71 (d, JH-P=3.0 Hz, 1H), 6.67 (d, 2.0 Hz, 1H), 3.89 (s, 3M), 3.63 (d, JH-P=11.2 Hz, 6H), 3.36 (d, JH-P=11.6 Hz, 6H), 2.02 (d, JH-P=2.5 Hz, 3H), 1.88 (d, JH-P=3.4 Hz, 3H), 1.38 (s, 9H). LC-MS: 3.26 min. (m/Z=407.1, 533.0, 555.0). It was noted that a faster-eluting undesirable isomeric side-product was also obtained during this reaction.

Provenance & Evidence