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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 417201생성일: 2026년 10월 24일

Diphenylphosphinic chloride → rac-(2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluoro-phenyl)-2'-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid (2-oxo-1,2-dihydro-pyridin-4-yl)-amide

https://huagongshe.com/ko/reaction/417201

반응식

참여 물질

역할이름HCID투입량
반응물Diphenylphosphinic chlorideHCID 73910—
반응물DiisopropylethylamineHCID 81531—
반응물4-Amino-1,2-dihydropyridin-2-oneHCID 573530—
반응물rac-(2'R,3'S,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluoro-phenyl)-2'-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid trifluoroacetic acidHCID 78158843—
용매1,2-DichloroethaneHCID 11—
생성물rac-(2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluoro-phenyl)-2'-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid (2-oxo-1,2-dihydro-pyridin-4-yl)-amideHCID 86653932—

반응 단계

In a manner similar to the method described in Example 27, rac-(2′S,3′R,4′S,5′R)-6-chloro-4′-(3-chloro-2-fluoro-phenyl)-2′-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3′-pyrrolidine]-5′-carboxylic acid trifluoroacetic acid prepared in Example 4 (0.45 g, 0.78 mmol), was reacted with diisopropylethylamine (0.8 g, 6.2 mmol), diphenylphosphinic chloride (0.74 g, 3.1 mmol), then reacted with 4-aminopyridin-2(1H)-one (Molbridge) (0.086 g, 0.78 mmol) in 1,2-dichloroethane at 60° C. to give rac-(2′S,3′R,4′S,5′R)-6-chloro-4′-(3-chloro-2-fluoro-phenyl)-2′-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3′-pyrrolidine]-5′-carboxylic acid (2-oxo-1,2-dihydro-pyridin-4-yl)-amide as a off white solid (Yield 28 mg, 6%).

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08088815B2
출처 데이터셋uspto-grants-2012_01
ORD IDord-929d9126e6a54124925ccd8076844a68
출처 메모uspto-grants-2012_01