Morpholine → HCID 58431155、化合物

To a solution of 1-{[(R)-7-(3,5-dichloro-phenyl)-5-methyl-6-oxo-5-(4-1,2,4-triazol-1-yl-benzyl)-6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carbonyl]-amino}-cyclopropanecarboxylic acid allyl ester (109 mg, 0.18 mmol) and morpholine (0.157 mL, 1.80 mmol) in 1 mL of THF was added Pd(Ph3P)4 (10 mg, 0.009 mmol). The reaction mixture was stirred at room temperature for 3 h. The reaction mixture was then diluted with 30 mL of EtOAc and washed with 10 mL each of 10% HCl solution, water, and brine, dried over Na2SO4, filtered, and concentrated to afford 114 mg of 1-{[(R)-7-(3,5-dichloro-phenyl)-5-methyl-6-oxo-5-(4-1,2,4-triazol-1-yl-benzyl)-6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carbonyl]-amino}-cyclopropanecarboxylic acid as an orange oily solid that was carried to the next step without further purification.

1. washwashed with 10 mL each of 10% HCl solution, water, and brine
2. dry with materialdried over Na2SO4
3. filtrationfiltered
4. concentrationconcentrated

ORDレコード

ord-5b979f9f9ff94eb8a799997d16dd8a3e

出典データセット

uspto-grants-2013_10

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08552205B2