CAS: 1148-11-4; Z-Pro-Oh

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Methyl (4S)-4-Azido-4-[(4S)-2,2-Dimethyl-1,3-Dioxolan-4-Yl]Butanoate置于palladium On Activated Charcoal Sodium Chlorite,Sodium Periodate,Disodium Hydrogenphosphate,氢气,二异丁基氢化铝,碳酸氢钠,溶剂黄146体系中,用 甲醇,乙醇,正己烷,甲苯,Petroleum Ether 用作溶剂,-78.0~25.0 °C,101.33 Kpa 条件下,反应 130.0H,反应生成N-苄氧羰基-L-脯氨酸
参考文献:Enantiospecific Syntheses Of (R)-And (S)-Proline And Some Derivatives From D-Glucono-1,5-Lactone
标题:Enantiospecific Syntheses Of (R)-And (S)-Proline And Some Derivatives From D-Glucono-1,5-Lactone
摘要:描述了从之前报道的 D-赤式己酸酯 9 中基于碳水化合物的对映特异性合成 (R)-脯氨酸 1 和 (S)-脯氨酸 2.对衍生自酯 9 的适当活化的中间体进行叠氮取代反应,然后进行还原环化 (H2/pd-C),得到取代的吡咯烷 14 和 22,它们以常规方式转化为相应的 N-Cbz 衍生物 16 和 24.将这些物质进行轻度酸性水解,然后氧化(偏高碘酸钠),得到受保护的脯氨酸 3 和 4,进一步氧化(亚氯酸钠),然后催化氢解,得到脯氨酸 1 和 2. N-Cbz-脯氨醇衍生物还报道了图5和图6.
Doi:10.1039/a704915C

专利信息

专利号:US-8426612-B2
优先权日:2009-04-22
标 题:Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole
发明人：SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO
权利人:SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO; ITALIANA SINT SPA
摘要:The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.

专利号:US-4727146-A
优先权日:1980-07-03
标题 :Synthesis of chiral 1-benzyl-1,2,3,4-tetra-hydroisoquinolines by asymmetric reduction
发明人：RICE KENNER C
权利人:US HEALTH
摘要:In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids. As a special function of this invention, certain of the derivatives, namely 4'-6' and 7'-9', may be hydrogenated to 1'-3' derivative by asymmetric reduction either of the catalytic or chemical type.

专利号:EP-3819295-A1
优先权日:2019-11-07
标 题 :Stereoselective synthesis of enantiomerically-enriched pantolactone
发明人：BONRATH WERNER; BOURGEOIS FREDERIC; MEDLOCK JONATHAN ALAN; SPARR CHRISTOF
权利人:DSM IP ASSETS BV
摘要:The present invention relates stereoselective synthesis of enantiomerically enriched pantolactone of formula (I) or (I').

专利号:US-4786684-A
优先权日:1986-08-21
标题 :Benzylthioether-linked solid support-bound thiol compounds and method for peptide synthesis
发明人：GLASS JOHN D
权利人:SINAI SCHOOL MEDICINE
摘要:A method for the synthesis of sulfydryl-containing peptides which comprises forming a benzylthioether-linked solid support-bound thiol compound having at least one functional group for generating at least one peptide bond, sequentially coupling at least one protected amino acid or peptide to the compound until a peptide having desired amino acid sequence is obtained, and cleaving the benzylthioether linkage to release the peptide from the support with concomitant regenertion of the sulfydryl group in the peptides. The invention also encompasses compounds having the general formula wherein X is H, NH2, or acyl-NHY, said acyl being an amino acid or a peptide; Y is H, COOH, CONHNH2, the ester COOR1 in which R1 is selected from the group consisting of methyl, ethyl, phenyl, ortho-nitrophenyl and para-nitrophenyl, the amide CONH2, or the amide CONHR2 in which R2 is an amino acid or peptide; and providing that X and Y cannot both be H.

专利号:US-6228988-B1
优先权日:1995-02-24
标题:Synthesis of hydroxamic acid derivatives
发明人：FLOYD CHRISTOPHER DAVID; LEWIS CHRISTOPHER NORMAN
权利人:BRITISH BIOTECH PHARM
摘要:The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group -CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1):where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.

专利号:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.