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HRID 72170作成日:2026年10月24日

N-Carbobenzoxy-L-valine → ((R)-3-{(S)-2-[(S)-2-((S)-2-Benzyloxycarbonylamino-3-methyl-butyrylamino)-3-methyl-butyrylamino]-3-methyl-butyrylamino}-2-hydroxy-propyl)-cyclohexylmethyl-phosphinic acid benzyl ester

https://huagongshe.com/ja/reaction/72170

反応式

関与物質

役割名称HCID仕込み量
反応物N-Carbobenzoxy-L-valineHCID 726987—
反応物{(R)-3-[(S)-2-((S)-2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-3-methyl-butyrylamino]-2-hydroxy-propyl}-cyclohexylmethyl-phosphinic acid benzyl esterHCID 68620254—
生成物((R)-3-{(S)-2-[(S)-2-((S)-2-Benzyloxycarbonylamino-3-methyl-butyrylamino)-3-methyl-butyrylamino]-3-methyl-butyrylamino}-2-hydroxy-propyl)-cyclohexylmethyl-phosphinic acid benzyl esterHCID 68621798—

反応手順

The resulting product from Step 1 was deprotected in a similar manner as Example 1, step 3, and the compound was used immediately and coupled to N-Cbz-L-valine in accordance with the procedures set forth in Example 12, Method B. The crude product was purified by gradient flash chromatography (methanol/methylene chloride) on a RediSep disposable column. 1H NMR (CD3Cl, 300 MHz): δ 7.45-7.25 (m, 10H), 6.0-5.85 (m, 1H), 5.18-4.92 (m, 4H), 4.50-4.33 (m, 2H), 4.31-4.04 (m, 2H), 3.43-3.26 (m, 2H), 2.25-2.03 (m, 3H), 2.02-1.70 (m, 8H), 1.37-1.10 (m, 4H), 1.04-0.82 (m, 20H). LCMS m/z: [M+H]+=757.9.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08828974B2
出典データセットuspto-grants-2014_09
ORD IDord-66d0a3bbbf7847b5886cbbd27d02ae96
出典メモuspto-grants-2014_09