Tert-Butyl D-Alaninate置于10% Nishimura Catalyst <(45.9% Rh/19.9% Pt) Oxide> 氢气体系中,用 甲醇 作为反应溶剂,25.0 °C,10.0 Mpa 条件下,反应 16.0H,反应生成 D-氨基丙醇 参考文献:Catalytic Hydrogenation Of Chiral α-Amino And α-Hydroxy Esters At Room Temperature With Nishimura Catalyst Without Racemization 标题:Catalytic Hydrogenation Of Chiral α-Amino And α-Hydroxy Esters At Room Temperature With Nishimura Catalyst Without Racemization 摘要:The Hydrogenation Or Carboxylic Acid Derivatives At Room Temperature Was Investigated. With A Mixed Rh/pt Oxide (Nishimura Catalyst),Low To Medium Activity Was Observed For Various Alpha-Amino And Alpha-Hydroxy Esters. At 100 Bar Hydrogen Pressure And 10% Catalysts Loading,High Yields Or Tire Desired Amino Alcohols And Diols Were Obtained Without Racemization. The Most Suitable Alpha-Substituents Were Nh2,Nhr,And 011,Whereas Beta-Nh2 Were Less Effective. Usually,Aromatic Rings Were Also Hydrogenated,But With The Free Bases Of Amino Acids As Substrates,Some Selectivity Was Observed. No Reaction Was Round For Alpha-Nr2,Alpha-Or,And Unfunctionalized Esters; Acids And Amides,Were Also Not Reduced Under These Conditions. A Working Hypothesis For The Mode Or Action Of The Catalyst Is Presented. DOI:10.1002/1615-4169(20011231)343:8<802::Aid-Adsc802>3.0.Co;2-T
专利号:US-10040752-B2 优先权日:2015-08-24 标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof 发明人:MKRTCHYAN GNEL; YAO QINGWEI 权利人:CODY LABORATORIES INC 摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.
专利号:US-2006058532-A1 优先权日:2004-09-10 标 题:Process for the scalable synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]-indole derivatives 发明人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 权利人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 摘要:The invention is directed to a process of synthesizing compounds of formula (VI): n n nwherein R 1- R 9 , R 3′ , R 4′ and Y are as set forth in the specification, and said method is useful for large scale synthesis thereof. The invention is also directed to useful intermediates for synthesizing the compounds of formula (VI) and processes of preparing said intermediates.
专利号:US-9394264-B2 优先权日:2009-11-13 标 题: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 权利人:RECEPTOS INC 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-11993577-B2 优先权日:2021-09-01 标 题 :Synthesis of MDMA or its optically active (R)- or (S)-MDMA isomers 发明人:FAWAZ MAJED; MORRA NICHOLAS 权利人:EMPATHBIO INC 摘要:Provided herein is a process for the preparation of 3,4-methylenedioxymethamphetamine, (R)-3,4-methylenedioxymethamphetamine and (S)-3,4-methylenedioxymethamphetamine.
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.
专利号:US-2025066313-A1 优先权日:2021-12-02 标 题 :Methods of Synthesis of Chiral 3,5-Disubstituted Morpholine Compounds and Intermediates Useful Therein 发明人:SUN YUANMING; ZHANG QIN; YANG JIANZHANG; XU ZHONGMIN; LAI XINZHONG; DEERBERG JOERG 权利人:BEIGENE SWITZERLAND GMBH 摘要:Provided herein are diastereomer-selective synthetic methods and intermediates for making chiral 3,5-disubstituted morpholine compounds, which are useful for the preparation of compounds useful as mitochondrial-derived activator of caspases (SMAC) mimetics for the treatment of proliferative diseases such as cancer.
摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 161. 摘要:Hollmann, F., Science of Synthesis Knowledge Updates, (2021) 3, 437. 参考文献:10.1063/1.2888562 摘要:Irrera S, Costa D. New insight brought by density functional theory on the chemical state of alaninol on Cu(100): energetics and interpretation of x-ray photoelectron spectroscopy data. J Chem Phys. 2008 Mar 21;128(11):114709. doi: 10.1063/1.2888562.