HRID69989

反应详情

EQUATION

反应方程式

REACTANTS

反应物

HCID70700873

6-Bromo-3-fluoropyridine-2-carboxylic acid

C6H3BrFNO2

结构：CC(C)(C)OC(=O)N[C@H]1C[C@@H](CO[Si](C)(C)C(C)(C)C)CN(c2ccncc2N)C1

HCID131731822

未命名化合物

PRODUCTS

生成物

结构：CC(C)(C)OC(=O)N[C@H]1C[C@@H](CO)CN(c2ccncc2NC(=O)c2nc(Br)ccc2F)C1

HCID131731823

未命名化合物

PROCEDURE

实验过程

Following Method 11 of Example 305, cis (+/−)-tert-butyl 1-(3-aminopyridin-4-yl)-5-((tert-butyldimethylsilyloxy)methyl)piperidin-3-ylcarbamate and 6-bromo-3-fluoropicolinic acid were coupled. Following purification by RP HPLC the product fractions were allowed to stand at it overnight in the 0.1% TFA acetonitile/water solution which removed the silyl group. Upon subsequent lyophilization, cis (+/−)-tert-butyl 1-(3-(6-bromo-3-fluoropicolinamido)pyridin-4-yl)-5-(hydroxymethyl)piperidin-3-ylcarbamate was obtained and used in Suzuki reactions directly. LCMS (m/z): 524.0/526.0 (MH+); LC Rt=2.90 min.

WORKUP

后处理

custompurification by RP HPLC the product fractions
customto stand at it overnight in the 0.1% TFA acetonitile/water solution which
customremoved the silyl group