专利号:US-11891375-B2 优先权日:2021-07-26 标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates 发明人:AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.
专利号:US-11274081-B2 优先权日:2016-05-30 标 题:Process for the synthesis of ivacaftor 发明人:REDDY DUMBALA SRINIVASA; KULKARNI AMOL ARVIND; NATARAJAN VASUDEVAN; SHARMA MRITYUNJAY KESHAVPRASAD 权利人:COUNCIL SCIENT IND RES 摘要:The present disclosed an improved process for the synthesis of ivacaftor starting from indole acetic acid ester which can be performed in batch as well as continuous flow synthesis. The present invention further disclosed to a continuous process for the synthesis of compound of formula (II) or formula (III) from compound of formula (I) in continuous flow reactor.
专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
专利号:US-7122693-B2 优先权日:1988-04-11 标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof 发明人:BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE 权利人:SHIRE BIOCHEM INC 摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.
专利号:US-8334381-B2 优先权日:2006-11-16 标题 :Process for the preparation of intermediates useful in the synthesis of imatinib 发明人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO 权利人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO; ITALIANA SINT SPA 摘要:It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.
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.
[参考文献]: Anirban Sarkar, Et Al. Lack Of Correlation Between Catalytic Efficiency And Basicity Of Amines During The Reaction Of Aryl Methyl Ketones With Dmf-Dma: An Unprecedented Supramolecular Domino Catalysis. Org Biomol Chem. 2012 Jan 14;10(2):281-6. [参考文献]: Brad S Lambert, Et Al. Anabolic Responses To Acute And Chronic Resistance Exercise Are Enhanced When Combined With Aquatic Treadmill Exercise. Am J Physiol Endocrinol Metab. 2015 Feb 1;308(3):E192-200. [参考文献]: C Freissinet, Et Al. Search For Evidence Of Life In Space: Analysis Of Enantiomeric Organic Molecules By N,N-Dimethylformamide Dimethylacetal Derivative Dependant Gas Chromatography-Mass Spectrometry. J Chromatogr A. 2010 Jan 29;1217(5):731-40. [参考文献]: C Rodier, Et Al. Chirality And The Origin Of Life: In Situ Enantiomeric Separation For Future Space Missions. Chirality. 2002 Jun;14(6):527-32. [参考文献]: Khadijah M Al-Zaydi, Et Al. Microwave Assisted Condensation Reactions Of 2-Aryl Hydrazonopropanals With Nucleophilic Reagents And Dimethyl Acetylenedicarboxylate. Molecules. 2007 Aug 24;12(8):2061-79.
合成参考文献
摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 851. 摘要:Snaith, J. S., Science of Synthesis Knowledge Updates, (2011) 2, 226. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 108. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 182. 摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 183.