专利号:US-10626091-B2 优先权日:2014-10-01 标 题 :Process for the preparation of enzalutamide 发明人:CHIVUKULA KAMESWAR RAO; KARUTURI VEERA VENKATESWARA RAO; BENDA SRINIVAS; ANKE RAMACHANDRA; GAJULA DHARMAPURI; MOTURU VENKATA RAMA KRISHNA MURTHY; INDUKURI VENKATA SUNIL KUMAR; GORANTLA SEETA RAMA ANJANEYULU; CHAVA SATYANARAYANA 权利人:LAURUS LABS LTD 摘要:The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.
专利号:EP-2284161-A1 优先权日:2009-07-21 标 题:Process for the preparation of riluzole 发明人:GATTI PIER ANDREA; ZACCHE MATTEO; Gerli Fulvio 权利人:EDMOND PHARMA SRL 摘要:A new and efficient process for the synthesis of Riluzole, a drug used to treat amyotrophic lateral sclerosis, is disclosed the process comprises the reaction 4-trifluoromethoxyaniline, a thiocyanate salt and an inorganic or organic oxidant in acetic acid solution.
专利号:RU-1773262-C 优先权日:1988-04-07 标 题 :Method for synthesis of nitromethane derivatives or theirs alkaline
专利号:US-4182877-A 优先权日:1976-05-12 标 题:Substituted anthranilates 发明人:HARRIS ROGER L N; HUPPATZ JOHN L; PHILLIPS JOHN N; WITRZENS BARBARA 权利人:COMMW SCIENT IND RES ORG 摘要:Anthranilic acid derivatives exhibiting fungicidal properties and useful as synthesis intermediates have the formula: I wherein R is selected from the group consisting of a hydrogen atom; a -COOR3 group and a -CH2OH group; R1 and R2 are the same or different and selected from the group consisting of a hydrogen atom and alkyl and cycloalkyl groups (provided that R1 and R2 are not both hydrogen atoms), or R1 and R2, together with the nitrogen atom to which they are attached, form a non-aromatic heterocyclic ring structure; R3 is selected from the group consisting of a hydrogen atom and an alkyl group; R4 is selected from the group consisting of a hydrogen atom, a halogen atom and a hydroxyl group; R6 is selected from the group consisting of a hydrogen atom and a halogen atom; and R5 is selected from the group consisting of a hydrogen atom, a halogen atom, and nitro, thiocyano and formyl groups. A process for production of these compounds by self-condensation of a substituted aminocrotonate by phosphorous oxychloride is also disclosed.
专利号:WO-9401445-A1 优先权日:1992-07-14 标 题:Base-protected nucleotide analogs with protected thiol groups 发明人:HANNA MICHELLE M 权利人:RES CORP TECHNOLOGIES INC 摘要:The present invention is directed to protected thio analogs of the pyrimidine and purine bases for syntheses of DNA and RNA by chemical or enzymatic methods. The subject analogs include reagents suitable for DNA or RNA synthesis via phosphoramidite, H-phosphonate or phosphotriester chemistry as well as reagents suitable for use by RNA and DNA polymerase, including thermostable polymerases employed by PCR or other nucleic acid amplification techniques. Methods of synthesizing the nucleotide analogs are also provided by the present invention. The nucleotide analogs of this invention can thus be incorporated into oligonucleotides or polynucleotides, deprotected and derivatized with a functional group. A method of synthesizing oligonucleotides with a functional group using the subject nucleotide analogs is also provided.
[参考文献]: Carlos Platas-Iglesias, Et Al. Lead(Ii) Thiocyanate Complexes With Bibracchial Lariat Ethers: An X-Ray And Dft Study. Inorg Chem. 2005 Apr 4;44(7):2224-33.
合成参考文献
摘要:Seiler, H.G., H. Sigel and A. Sigel (eds.). Handbook on the Toxicity of Inorganic Compounds. New York, NY: Marcel Dekker, Inc. 1988., p. 843 摘要:USEPA/Office of Water; Federal-State Toxicology and Risk Analysis Committee (FSTRAC). Summary of State and Federal Drinking Water Standards and Guidelines (11/93) To Present 摘要:40 CFR 261.24 (USEPA); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of November 2, 2009: 摘要:50 CFR 20.134(b) (5) (United States Fish and Wildlife Service, Department of the Interior); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of October 30, 2009: https://www.ecfr.gov