专利号:US-2012203004-A1 优先权日:2009-08-13 标题 :process for the synthesis of alkyl/aralkyl (2s)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof: key intermediates for the preparation of dppiv inhibitors 发明人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA 权利人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA; LUPIN LTD 摘要:An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DP-PIV) inhibitors.
专利号:WO-2007054668-A1 优先权日:2005-11-09 标 题:Synthesis of methylsulphonyl benzene compounds 发明人:FISHER RAYMOND 权利人:PEAKDALE MOLECULAR LTD; FISHER RAYMOND 摘要:The present invention relates to a process for the synthesis of l-substituted-2-fluoro-4- methylsulfonylphenyl compounds.
专利号:US-7339065-B2 优先权日:2003-07-21 标题 :Design and synthesis of optimized ligands for PPAR 发明人:AVERY MITCHELL A; PERSHADSINGH HARRIHAR A 权利人:BETHESDA PHARMACEUTICALS INC; UNIV MISSISSIPPI 摘要:This invention provides new chemical entities useful for treating a variety of clinical disorders including those that are influenced by the activity of peroxisome proliferator activated receptors (PPAR). The structures of the compounds and methods to design, make and use the compounds are provided. Compounds and methods for administering therapeutic compositions comprising the compounds in cases of the disease psoriasis are provided. An exemplary compound having the formula compound is 5adamantan-2-yl-pentanoic acid {2-[4-(2,4-dioxo-thiazolidin-5-yl-methyl)-phenoxy]-ethyl}-methyl-amide is provided.
专利号:US-4592902-A 优先权日:1985-02-26 标题:Synthesis of crystalline silicate ZSM-5 with an alkyltropinium compound promoter 发明人:VALYOCSIK ERNEST W 权利人:MOBIL OIL CORP 摘要:There is provided a method and a reaction mixture for preparing crystalline silicate having the structure of ZSM-5 with an alkyltropinium directing agent, alkyl being of 2 to 5 carbon atoms.
专利号:WO-2024003151-A1 优先权日:2022-06-28 标 题:Chemical synthesis platform 发明人:CRONIN LEROY 权利人:UNIV GLASGOW COURT 摘要:The invention relates to a method for generating a database for chemical syntheses and a method for performing a chemical synthesis using a database. The method for generating a database comprises generating a series of instruction sets for a series of chemical syntheses from the literature, wherein each instruction set is a machine readable and executable universal language for a chemical synthesiser; assembling the series of instructions sets within a database, and making the instruction sets available for access and autonomous execution by a chemical synthesiser. The method for performing a chemical synthesis comprises accessing an instruction set from a database, providing the instruction set to a chemical synthesiser, and autonomously executing the instruction set on the chemical synthesiser thereby to perform the chemical synthesis. The invention makes use of a standardised and step-focussed syntax to describe the chemical syntheses, and a universal synthesis automation platform.
专利号:US-2023416243-A1 优先权日:2020-11-06 标 题 :Process for Preparing Heterocyclic Methanone Compounds and AZA-Bicyclo Intermediates Thereof 发明人:GRUGEL CHRISTIAN 权利人:ACTINOGEN MEDICAL LTD 摘要:The present disclosure relates to a process for synthesis of heterocyclic methanone compounds, and in particular 3′-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds, and aza-bicyclo intermediates thereof. In particular, the present disclosure also relates to a process for the synthesis of Xanamem. The present disclosure also relates to a process for the synthesis of optionally protected aza-bicyclo intermediate compounds. The present disclosure also relates to 3′-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and aza-bicyclo intermediate compounds thereof.
[参考文献]: Bedewitz Ma, Et Al. Tropinone Synthesis Via An Atypical Polyketide Synthase And P450-Mediated Cyclization. Nat Commun. 2018 Dec 11;9(1):5281. Doi: 10.1038/s41467-018-07671-3. [参考文献]: Beata Kolesińska, Et Al. An Approach For Synthesis Of Tropinone Analogue N-Substituted With Triazine Ring. Acta Pol Pharm. 2008 Nov-Dec;65(6):749-51. [参考文献]: Henning Steen, Et Al. Images In Cardiovascular Medicine. A Rare Form Of Midventricular Tako-Tsubo After Emotional Stress Followed Up With Magnetic Resonance Imaging. Circulation. 2006 Aug 15;114(7):E248. [参考文献]: John A Porco Jr, Et Al. Organic Chemistry: Synthesis Undressed. Nature. 2007 Mar 22;446(7134):383-5. [参考文献]: K Nakajima, Et Al. Crystal Structures Of Two Tropinone Reductases: Different Reaction Stereospecificities In The Same Protein Fold. Proc Natl Acad Sci U S A. 1998 Apr 28;95(9):4876-81.
合成参考文献
摘要:Nieto, C. T.; Eames, J.; Garrido, N. M., Science of Synthesis Knowledge Updates, (2019) 1, 117. 摘要:Scammells, P. J., Science of Synthesis Knowledge Updates, (2013) 2, 429. 摘要:Scammells, P. J., Science of Synthesis Knowledge Updates, (2013) 2, 436. 摘要:Li, H.; Wang, Y.; Liu, Q., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 511. 参考文献:10.1007/s10822-006-9037-3 摘要:Miguet L, Zhang Z, Barbier M, Grigorov MG. Comparison of a homology model and the crystallographic structure of human 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) in a structure-based identification of inhibitors. J Comput Aided Mol Des. 2006 Feb;20(2):67–81. doi: 10.1007/s10822-006-9037-3.