N-羟基丁二酰亚胺,氯甲酸三氯甲酯置于乙腈体系中,化学反应 0.17H,以affording 6.5 G Of The Titled Compound In The Form Of Colorless Crystals的收率获得产物n,N'-二琥珀酰亚胺基碳酸酯 参考文献:Imido Carbonate Compound,Production Thereof And Uses Thereof As Reagent 标题:Imido Carbonate Compound,Production Thereof And Uses Thereof As Reagent 摘要:一种新的碳酸盐化合物,其为n,N'-二琥珀酰亚胺基碳酸酯,N,N'-二邻苯二甲酰亚胺基碳酸酯或n,N'-双(5-壬烯-2,3-二羧酰亚胺基)碳酸酯,通过将化合物r-Oh(其中r为琥珀酰亚胺基,邻苯二甲酰亚胺基或5-壬烯-2,3-二羧酰亚胺基)的n-羟基化合物与硅烷化剂反应,然后将所得的硅烷化产物与光气反应而制得,或者通过将所述n-羟基化合物与三氯甲基氯甲酸酯在熔融状态下或在非极性有机溶剂(例如二甲苯)的存在下反应而制得.这种新的碳酸盐化合物不仅可用作从氨基酸形成活性酯的试剂,还可用作在一对氨基基团,一对氨基和羟基基团或一对氨基和巯基基团之间引入羰基基团的试剂,通过从二硫代氨基甲酸中去除硫化氢来反应生成异硫氰酸盐,以及通过脱水n-保护丝氨酸来产生丙烯酸衍生物.
专利号:US-2022298204-A1 优先权日:2019-07-05 标题 :Synthesis of a-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:US-9233943-B2 优先权日:2012-01-10 标题:Process for synthesis of syn azido epdxide and its use as intermediate for the synthesis of amprenavir and saquinavir 发明人:GADAKH SUNITA KHANDERAO; REKULA REDDY SANTHOSH; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:A novel synthetic route to the syn-azido epoxide of formula 5 includes cobalt-catalyzed hydrolytic kinetic resolution of a racemic mixture of the azido-epoxide. Reaction steps include subjecting an allylic alcohol to epoxidation with mCPBA to obtain a racemic epoxy alcohol; ring opening the epoxy alcohol with azide anion to obtain an anti-azido alcohol, which can then be selectively tosylated at the primary alcohol; treating the tosylate with base to obtain the racemic azido-epoxide; and subjecting the racemic azido-epoxide to cobalt-catalyzed hydrolytic kinetic resolution to obtain the syn-azido epoxide of formula 5. The compound of formula 5 may be used as a common intermediate for the asymmetric synthesis of HIV protease inhibitors, such as Amprenavir, Fosamprenavir, Saquinavir, and formal synthesis of Darunavir and Palinavir.
专利号:US-11059849-B2 优先权日:2014-09-02 标题 :Modified nucleotides for synthesis of nucleic acids, a kit containing such nucleotides and their use for the production of synthetic nucleic acid sequences or genes 发明人:YBERT THOMAS; GARIEL SYLVAIN 权利人:DNA SCRIPT 摘要:A modified nucleotide, intended for the synthesis of long chain nucleic acids by enzymatic processes, comprising a “naturalâ€? nitrogenous base or a natural nitrogenous base analogue, a ribose or deoxyribose carbohydrate, and at least one phosphate group, characterized in that said nucleotide comprises at least one R group, termed the modifier group, carried by said nitrogenous base or analogue and/or by the oxygen in position 3′ of the ribose or deoxyribose molecule, making it possible to block the polymerization of said nucleotide and/or to allow the interaction of said nucleotide with another molecule, such as a protein, during the nucleic acid synthesis, R comprising at least one functional terminal group.
专利号:EP-3792250-A1 优先权日:2019-09-13 标题:Synthesis of alpha-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:US-11447454-B2 优先权日:2015-08-07 标题:Synthesis of benzodiazepine derivatives 发明人:BOYCE MALCOLM JAMES; THOMSEN LIV; GILBERT DONALD ALAN; WOOD DAVID 权利人:TRIO MEDICINES LTD 摘要:The invention relates to processes for the synthesis of benzodiazepine derivatives of Formula I:
专利号:US-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
[参考文献]: Boontida Morakul, Et Al. Dissolution Enhancement And In Vitro Performance Of Clarithromycin Nanocrystals Produced By Precipitation-Lyophilization-Homogenization Method. Eur J Pharm Biopharm. 2014 Nov;88(3):886-96. [参考文献]: Christian Hermansen, Et Al. Structure-Topology-Property Correlations Of Sodium Phosphosilicate Glasses. J Chem Phys. 2015 Aug 14;143(6):064510. [参考文献]: Haiqiang Cao, Et Al. Codelivery Of Sorafenib And Curcumin By Directed Self-Assembled Nanoparticles Enhances Therapeutic Effect On Hepatocellular Carcinoma. Mol Pharm. 2015 Mar 2;12(3):922-31. [参考文献]: Kimberly J Hassett, Et Al. Glassy-State Stabilization Of A Dominant Negative Inhibitor Anthrax Vaccine Containing Aluminum Hydroxide And Glycopyranoside Lipid A Adjuvants. J Pharm Sci. 2015 Feb;104(2):627-39. [参考文献]: Luz María Martínez, Et Al. Stabilization Of Amorphous Paracetamol Based Systems Using Traditional And Novel Strategies. Int J Pharm. 2014 Dec 30;477(1-2):294-305.
合成参考文献
摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 115. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 参考文献:10.1016/j.jasms.2008.02.004 摘要:Jalili PR, Ball HL. Novel reversible biotinylated probe for the selective enrichment of phosphorylated peptides from complex mixtures. Journal of The American Society for Mass Spectrometry. 2008 May;19(5):741–50. doi: 10.1016/j.jasms.2008.02.004. 参考文献:10.1007/s00216-019-01892-1 摘要:Chekin F, Mishyn V, Barras A, Lyskawa J, Ye R, Melinte S, Woisel P, Boukherroub R, Szunerits S. Dopamine-functionalized cyclodextrins: modification of reduced graphene oxide based electrodes and sensing of folic acid in human serum. Analytical and Bioanalytical Chemistry. 2019 Jun 27;411(20):5149–57. doi: 10.1007/s00216-019-01892-1.