Water → HCID 58529667、化合物

温度

110 °C

To a solution of tert-butyl 4-(4-amino-5-bromopyrrolo[2,1-f][1,2,4]triazin-7-yl)piperidine-1-carboxylate (0.5 g, 1.26 mmol) in DMF (15 mL) was added 2-(2-fluorobenzyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2H-indazol-3-amine (0.695 g, 1.89 mmol), solid Na2CO3 (0.4 g, 3.79 mmol) and water (1.9 mL). The solution was degassed for 10 min and tetrakis(triphenylphosphine)palladium(0) (0.146 g, 0.126 mmol) was added and the mixture was degassed for another 10 min. The mixture was heated at 110° C. for 1 h 15 min and then cooled to rt. The mixture was filtered through a plug of Celite® and the filtrate was concentrated. The crude purified using an ISCO® instrument using 40-100% ethyl acetate in hexanes. LC-MS [M+H]+=557.2, RT=2.65 min.

1. customThe solution was degassed for 10 min
2. customthe mixture was degassed for another 10 min
3. temperaturecooled to rt
4. filtrationThe mixture was filtered through a plug of Celite®
5. concentrationthe filtrate was concentrated
6. customThe crude purified

ORDレコード

ord-26d11e9e3d8e4144b7bb4e54e653fa67

出典データセット

uspto-grants-2013_04

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08431695B2