CAS: 61341-86-4; (S)-2,3-Dihydro-1H-Inden-1-Amine

上下游产品

1-茚酮置于palladium On Activated Charcoal,镍 氢气,对甲苯磺酸,溶剂黄146体系中,用 乙醇,醋酸异丙酯 作为反应溶剂,40.0 °C,500.0 Kpa 条件下,反应 51.0H,反应生成 (S)-(+)-1-氨基茚满
参考文献:(S)-1-氨基茚满:以(R)-苯基甘氨酸酰胺为手性助剂,通过手性转移合成
标题:(S)-1-氨基茚满:以(R)-苯基甘氨酸酰胺为手性助剂,通过手性转移合成
摘要:已经开发了一种实用的不对称合成的近对映体纯的(S)-1-氨基茚满.关键步骤涉及使用手性助剂(R)-苯基甘氨酸酰胺的非对映选择性金属催化的1-茚满酮的酮亚胺还原.关于金属催化剂,溶剂和催化剂负载量,优化了不对称氢化步骤的选择性.通过新型的非还原性方法除去手性助剂.因此,在有效的三步法中,由(R)-苯基甘氨酸酰胺以58%的总收率制备了ee为96%的(S)-1-氨基茚满.
DOI:10.1016/j.Tetasy.2003.08.040

专利信息

专利号:US-10189803-B2
优先权日:2008-02-22
标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
发明人：CHONG HYUN-SOON
权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH
摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

专利号:US-7452994-B2
优先权日:2001-09-12
标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
发明人：MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN
权利人:ANORMED INC
摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.

专利号:US-8084630-B2
优先权日:2007-05-31
标 题 :Process for the synthesis of ramelteon and its intermediates
发明人：KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL
权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL; TEVA PHARMA
摘要:The present invention provides processes and intermediates for the synthesis of ramelteon.

专利号:US-7109377-B2
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
发明人：SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R
权利人:HARVARD COLLEGE
摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

专利号:US-9388147-B2
优先权日:2009-11-13
标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis
发明人：MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN
权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL
摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.