专利号:US-11040938-B2 优先权日:2016-07-27 标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts 发明人:MA BING; PAN SHUAI 权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH 摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:WO-2025108921-A1 优先权日:2023-11-22 标 题 :Synthesis of radiopharmaceutical agents 发明人:AUZELOUX PHILIPPE; LEVESQUE SOPHIE; GALMIER MARIE-JOSÈPHE; CHEZAL JEAN-MICHEL 权利人:INST NAT SANTE RECH MED; UNIV CLERMONT AUVERGNE; CENTRE LUTTE CONTRE LE CANCER 摘要:Synthesis of radiopharmaceutical agents It is disclosed a method to synthesize a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I), (I) said process comprising contacting a trialkylstannane precursor of formula (II), or a pharmaceutically acceptable salt thereof: Formula (II), (II) with an alkali metal salt of a radionuclide selected from the group consisting of 123I, 124I, 125I, 131I, 211At, in appropriate acidic conditions and in presence of a peroxide ROOH in an 10 appropriate concentration. Said method is particularly suited for synthesizing [131I]N-(2- diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide, providing a notable reduction in the quantity of side products, allowing a much purer finished product, while making use of reagents which are adapted to the constraints which need to be met when developing a product for clinical use and, more in particular, to the constraints to be met in order to 15 adapt the process for being fully automated.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-12018313-B2 优先权日:2016-12-28 标题:Methods, apparatuses, and systems for microorganism strain analysis of complex heterogeneous communities with tracer analytics, determination of functional relationships and interactions thereof, and synthesis of microbial ensembles 发明人:EMBREE MALLORY 权利人:NATIVE MICROBIALS INC 摘要:Methods, apparatuses, and systems for microorganism strain analysis of complex heterogeneous communities with tracer analytics, determination of functional relationships and interactions thereof, and synthesis of microbial ensembles, including dosed microbial ensembles and inoculative microbial ensembles, are disclosed.
专利号:WO-2025104624-A1 优先权日:2023-11-14 标题 :Synthesis of 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1h-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-d-threo-pentitol 发明人:ALEXANDER KATY LOUISE; ANSARI ZARRIN FAZAL KHADIJA; DANIELS DAVID SYDNEY BERNARD; HASSEL LUKE HARRY; KEEN STEPHEN PHILIP; SCOTT JEREMY PETER; SCOTT REUBEN JOHN; SIMMONS JOHATHAN ANDREW; STOLL EMMA LOUISE; TRINDADE ALEXANDRE FONSECA; VICINI ANNA CHIARA 权利人:PFIZER 摘要:This disclosure relates novel methods to prepare 1,5-anhydro-3-({5-chloro-4-[4- fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2- yl}amino)-2,3-dideoxy-D-threo-pentitol, and hydrates and stereoisomers thereof, as well as intermediates, including solid forms of the intermediates, useful for the preparation of such compounds and the synthesis of said intermediates.
专利号:US-6455680-B1 优先权日:2000-12-21 标 题 :Methods utilizing aryl thioimines in synthesis of erythromycin derivatives 发明人:LUKIN KIRILL A 权利人:ABBOTT LAB 摘要:An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
摘要:Lewis, R.J. Sr.; Hawley's Condensed Chemical Dictionary 15th Edition. John Wiley & Sons, Inc. New York, NY 2007., p. 1033 摘要:Gosselin, R.E., R.P. Smith, H.C. Hodge. Clinical Toxicology of Commercial Products. 5th ed. Baltimore: Williams and Wilkins, 1984., p. II-123 摘要:Barbera JJ et al; Ullmann's Encyclopedia of Industrial Chemistry 7th ed. (2010). NY, NY: John Wiley & Sons; Sulfites, Thiosulfates, and Dithionites. Online Posting Date: June 15, 2000 摘要:O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Whitehouse Station, NJ: Merck and Co., Inc., 2006., p. 1318 摘要:WHO/FAO; Joint Expert Committee on Food Additives (JECFA): Food Additive Series 42: Preservative: Sulfur dioxide and sulfites (WHO Food Additives Series 42). Available from, As of July 28, 2011: