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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 1433791생성일: 2026년 10월 27일

(2S,3R)-3-(benzyloxy)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)butanoic acid → (3S)-N-(4-Ethynyl-2-fluoro-phenyl)-2-{(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl}-3-phenyl-butyramide

https://huagongshe.com/reaction/1433791

반응식

참여 물질

역할이름HCID투입량
반응물(2S,3R)-3-(benzyloxy)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)butanoic acidHCID 16213170—
반응물(2S,3S)-2-amino-N-(2-fluoro-4-iodo-phenyl)-3-phenyl-butyramideHCID 68618997—
반응물(2S,3S)-2-{(R)-2-amino-2-[4-((R)-2,3-dihydroxy-propoxy)-phenyl]-acetylamino}-N-(2-chloro-4-iodo-phenyl)-3-phenyl-butyramideHCID 69006543—
반응물(2S, 3S)-2-amino-N-(2-fluoro-4-trimethylsilanylethynyl-phenyl)-3-phenyl-butyramideHCID 69007467—
생성물(3S)-N-(4-Ethynyl-2-fluoro-phenyl)-2-{(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl}-3-phenyl-butyramideHCID 57935085—

반응 단계

Prepared by the same method as described in example 48 except that (i) after step 3, and prior to step 4, (2S,3S)-2-amino-N-(2-fluoro-4-iodo-phenyl)-3-phenyl-butyramide was converted to (2S,3S)-2-amino-N-(2-fluoro-4-trimethylsilanylethynyl-phenyl)-3-phenyl-butyramide under the conditions described below, and (ii) after initial purification in step 6 the product was subjected to chiral HPLC separation as described below. The trimethylsilyl group introduced in step 3 was subsequently removed during step 5 of the synthesis, concomitant with removal of the tert-butyloxycarbonyl protecting group.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US07612212B2
출처 데이터셋uspto-grants-2009_11
ORD IDord-967bdf41824e468bbf445ec54d7e36c4
출처 메모uspto-grants-2009_11