专利号:US-6982350-B2 优先权日:2004-05-19 标 题:Process for the synthesis of (1S)-4,5-dimethoxy-1-(methylaminomethyl)-benzocyclobutane and addition salts thereof, and to the application thereof in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:LERESTIF JEAN-MICHEL; GONZALEZ BLANCO ISAAC; LECOUVE JEAN-PIERRE; BRIGOT DANIEL 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
专利号:US-10456387-B2 优先权日:2011-11-29 标 题:Phacetoperane for treating of attention deficit hyperactivity disorder 发明人:KONOFAL ERIC; FIGADERE BRUNO 权利人:NLS PHARMA AG; NLS PHARMACEUTICS AG 摘要:The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane.
专利号:US-8846916-B2 优先权日:2009-05-11 标题:Sitagliptin synthesis 发明人:GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH 权利人:GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH; GENERICS UK LTD 摘要:The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.
专利号:US-6380416-B2 优先权日:1997-06-13 标题:Asymmetric synthesis catalyzed by transition metal complexes with rigid chiral ligands 发明人:ZHANG XUMU 权利人:PENN STATE RES FOUND 摘要:This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral bidentate phosphine ligands with cyclic ring structures which could be used to restrict conformational flexibility of the ligands and thus the efficiency of chiral transfer can be enhanced through the ligand rigidity.
专利号:WO-2016192694-A1 优先权日:2015-06-05 标 题 :A process for preparing the key intermediate of apremilast, using enzymatic resolution of the racemic amines 发明人:DOUBSKY JAN; KLVANA ROBERT; RICHTER JINDRICH; Lehnert Petr 权利人:ZENTIVA KS 摘要:The invention relates to a preparation method of (S)-l-(3-ethoxy-4-methoxyphenyl)- 2-(methylsulfonyl)-ethyl-amine (S)-l, or its N-acyl derivatives of general formula (S)-2. The amine (S)-l is the key intermediate in the synthesis of (S)-{2-[l-(3-ethoxy-4- methoxyphenyi)-2-methyisulfonylethyl]-4-acetylaminoisoindolin-l ?3-dione, known as Apremilast. In this synthesis, the amine (S)-l, or its respective salts, are subjected to condensation with 3-acetamidophthalic anhydride 4, providing the desired product 3 (Scheme 1).
1: LEAU O, DUCROT R. [Action of acetylleucine on experimental vertigo in mice]. C R Seances Soc Biol Fil. 1957;151(7):1365-7. French.
合成参考文献
摘要:Faber, K.; Glueck, S. M., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 441. 摘要:CELICE J, LEAU O, DUCROT R, DUCHESNAY G. [Trial therapy of labyrinthine vertigo by acetyl-DL-leucine]. Therapie. 1958;13(4):620–7.