专利号:US-8927739-B2 优先权日:2011-05-18 标 题 :Processes for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives 发明人:QIU YAO-LING; PENG XIAOWEN; KIM IN JONG; CAO HUI; TANG DATONG; OR YAT SUN; WANG GUOQIANG; XU GUOYOU 权利人:ENANTA PHARM INC 摘要:The present invention relates generally to an improved process for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of hepatits C virus NS5A inhibitors. In particular, the present invention relates to processes and intermediates for the preparation of compounds of formulae (Ia), (Ib) and (Ic):
专利号:US-6288297-B1 优先权日:1998-10-01 标 题:Process for the preparation of cyclopropylacetylene 发明人:WANG ZHE; YIN JIANGUO; FORTUNAK JOSEPH M; CAMPAGNA SILVIO 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn is hydroxy protected to form 1,1,1-trichloro-2-cyclopropylethyltosylate; which in turn undergoes elimination to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.
专利号:US-8129560-B2 优先权日:2005-08-15 标 题 :Process for the synthesis of mandipropamid and derivatives thereof 发明人:BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG 权利人:BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG; SYNGENTA CROP PROT INC 摘要:A process for the preparation of a compound of formula (I), the process comprising: (i) the reaction of a compound of formula (III), with a compound of formula (IV) to give a compound of formula (II), and (ii) the reaction of the compound of formula (II) with a leaving group, to give the compound of formula (I).
专利号:US-3708547-A 优先权日:1969-09-02 标 题 :Synthesis of(10)-annulenes 发明人:NELSON P; UNTCH K 权利人:SYNTEX CORP 摘要:NEW PROCESS FOR PREPARING (10)-ANNULENE COMPOUNDS WHICH ARE USEFUL AS ESTROGENIC, ANTI-INFLAMMATORY, AND ANTI-FERTILITY AGENTS. THE PROCESS UTILIZES THE STEPS OF ADDING A METHANO, DICHLOROMETHANO, OR DIFLUOROMETHAO GROUP ACROSS THE C-9,10 DOUBLE BOND OF A 1,4,5,8-TETRAHYDRONAPHTHALENE TO THE CORRESPONDIG 9,10-BRIDGED-1,45,8,9,10-HEXAHYDRONAPHTHLENE AND TREATING THE LATTER WITH A BENZOQUINONE TO THE CORRESPONDING 1,6-BRIDGED(10)-ANNULENE PRODUCT. THE PREPARATINS OF 1,6-METHANO(10)-ANNULENE, 1,6-DICHLOROMETHANO-(10)-ANNULENE, AND 1,6-DIFLUOROMETHANE-(10)-ANNULENE ARE ILLUSTRATED AS REPRESENSTATIVE OF THE PROCESS.
专利号:US-6359164-B1 优先权日:1998-10-01 标 题:Process for the preparation of cyclopropylacetylene 发明人:WANG ZHE; FORTUNAK JOSEPH M 摘要:The present invention relates generally to novel methods for the preparation of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor with superior anti-retroviral activity. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn undergoes elimination to form 1,1-dichloro-2-cyclopropyl-ethene; which in turn undergoes elimination to form cyclopropyl acetylene.
专利号:US-8921573-B2 优先权日:2011-10-18 标 题:Processes for the preparation of novel benzimidazole derivatives 发明人:TANG DATONG; XU GUOYOU; PENG XIAOWEN; YING LU; WANG CE; CAO HUI; LONG JIANG; KIM IN JONG; WANG GUOQIANG; QIU YAO-LING; OR YAT SUN 权利人:ENANTA PHARM INC 摘要:The present invention relates to processes and intermediates for the preparation of novel benzimidazole derivatives, especially in the synthesis of hepatitis C virus NS5A inhibitors. In particular, the present invention relates to processes and intermediates for the preparation of compounds of formulae (I-a):
[参考文献]: Adhiraj Roy, Et Al. Assessing Glucose Uptake Through The Yeast Hexose Transporter 1 (Hxt1). Plos One. 2015 Mar 27;10(3):E0121985. [参考文献]: Alessia Finotti, Et Al. Erythroid Induction Of K562 Cells Treated With Mithramycin Is Associated With Inhibition Of Raptor Gene Transcription And Mammalian Target Of Rapamycin Complex 1 (Mtorc1) Functions. Pharmacol Res. 2015 Jan:91:57-68. [参考文献]: Alessia Landi, Et Al. Genome-Wide Shrna Screening Identifies Host Factors Involved In Early Endocytic Events For Hiv-1-Induced Cd4 Down-Regulation. Retrovirology. 2014 Dec 13:11:118. [参考文献]: Bastian Mühl, Et Al. Spreds (Sprouty Related Proteins With Evh1 Domain) Promote Self-Renewal And Inhibit Mesodermal Differentiation In Murine Embryonic Stem Cells. Dev Dyn. 2015 Apr;244(4):591-606. [参考文献]: César Pedroza-Roldán, Et Al. The Adenylyl Cyclase Rv2212 Modifies The Proteome And Infectivity Of Mycobacterium Bovis Bcg. Folia Microbiol (Praha). 2015 Jan;60(1):21-31.
合成参考文献
摘要:Jurez P; Arch Insect Biochem Physiol 25 (3): 177-91 (1994) 摘要:Gerhartz, W. (exec ed.). Ullmann's Encyclopedia of Industrial Chemistry. 5th ed.Vol A1: Deerfield Beach, FL: VCH Publishers, 1985 to Present., p. VA3 528 摘要:NIOSH; National Occupational Exposure Survey (NOES) (1983) 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 摘要:IARC. Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Humans. Geneva: World Health Organization, International Agency for Research on Cancer, 1972-PRESENT. (Multivolume work).