Реакция #2146764

ord-3d68a0efefe943b19d2d0cc2149b6084

Уравнение реакции

CC(C)(C)OC(=O)N1CCC(Oc2cc3ccnc(OCc4ccccc4)c3cc2Cl)CC1
4-(1-Benzyloxy-7-chloro-isoquinolin-6-yloxy)-piperidine-1-carboxylic acid tert-butyl-ester
Cl.O=c1[nH]ccc2cc(OC3CCNCC3)c(Cl)cc12
desired compound
Выход 69.6%
Cl.O=c1[nH]ccc2cc(OC3CCNCC3)c(Cl)cc12
7-Chloro-6-(piperidin-4-yloxy)-2H-isoquinolin-1-one-hydrochloride
Выход 69.6%

Растворители

Условия реакции

Подробные условия
See reaction.notes.procedure_details.

Обработка

  1. 1
    ДругоеThe solvent was removed i
  2. 2
    Другоеand the residue was purified by preparative HPLC
  3. 3
    ДругоеThe product fractions were evaporated
  4. 4
    workup.DISSOLUTIONdissolved in 2 N HCl

Методика

254 mg (0.52 mmol) of 4-(1-Benzyloxy-7-chloro-isoquinolin-6-yloxy)-piperidine-1-carboxylic acid tert-butyl-ester (6) were stirred in methanol/2 N HCl (1:1) at room temperature overnight. The solvent was removed i. vac. and the residue was purified by preparative HPLC. The product fractions were evaporated and dissolved in 2 N HCl. Lyophilization results in 57 mg of the desired compound. Rt=0.95 min (Method B). Detected mass: 279.1 (M+H+).

Источник

DOI: 10.6084/m9.figshare.5104873.v1Патент: US08278294B2uspto-grants-2012_10