CAS: 694-87-1; Bicyclo[4.2.0]Octa-1,3,5-Triene

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1-Fluoro-2-(2-Iodoethyl)Benzene置于甲醇,叔丁基锂体系中,用 四氢呋喃,乙醚,正戊烷 作为反应溶剂,以45%的收率获得产物苯并环丁烯
参考文献:苯炔系烷基锂的环化:3-取代的苯并环丁烯和5-取代的四氢萘的制备
标题:苯炔系烷基锂的环化:3-取代的苯并环丁烯和5-取代的四氢萘的制备
摘要:由适当的α-(2-氟苯基)-ω-碘代烷烃以20-40%的收率进行五步一锅法制备的异构体纯净的3-取代的苯并环丁烯或5-取代的四氢萘,涉及反应生成及随后的4-或6-外一个苯炔拴烷基锂的环化,进行说明.
DOI:10.1016/s0040-4039(99)01434-3

专利信息

专利号:US-8288581-B2
优先权日:2008-07-17
标 题:Process for the preparation of functionalised benzocyclobutenes, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
发明人：PEGLION JEAN-LOUIS; BAUDOIN OLIVIER; AUDIC NICOLAS; CHAUMONTET MANON; PICCARDI RICCARDO
权利人:PEGLION JEAN-LOUIS; BAUDOIN OLIVIER; AUDIC NICOLAS; CHAUMONTET MANON; PICCARDI RICCARDO; SERVIER LAB; CENTRE NAT RECH SCIENT
摘要:Process for the preparation of compounds of formula (IV): n nwherein R 1 -R 6 are as defined in the specification.n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

专利号:US-8729310-B2
优先权日:2009-09-22
标题:Halogenated diarylamine compound and synthesis method thereof
发明人：OSAKA HARUE; INOUE HIROTO
权利人:OSAKA HARUE; INOUE HIROTO; SEMICONDUCTOR ENERGY LAB
摘要:An object is to provide a new halogenated diarylamine compound serving as a source material for synthesis of a variety of diarylamine compounds and triarylamine compounds and a synthesis method of the new halogenated diarylamine compound. A halogenated diarylamine compound represented by the following general formula (G1) and a synthesis method thereof are provided. Note that a variety of diarylamine compounds and triarylamine compounds can be synthesized using the halogenated diarylamine compound represented by the following general formula (G1).

专利号:US-4183864-A
优先权日:1978-02-21
标题:Cobalt catalyzed steroid synthesis
发明人：FUNK RAYMOND L; VOLLHARDT K PETER C
权利人:U S OF AMERICA HEW SECRETARY
摘要:Steroid compounds obtained by co-oligomerization of a side chain functionalized 1,5-hexadiyne with bis(trimethylsilyl)acetylene catalyzed by cyclopentadiene cobalt dicarbonyl, CpCO(CO) 2 , via intermediate benzocyclobutene formation followed by intramolecular cycloaddition to the sterospecific formation of the steroid nucleus. This constitutes a short steroid synthesis, five steps from commercially available acyclic precursor 1,5-hexadiyne and three steps from 2-methyl-cyclopent-2-enone.

专利号:US-12115510-B2
优先权日:2019-10-09
标题:High surface area coatings for solid-phase synthesis
发明人：NGUYEN BICHLIEN HOANG; STRAUSS KARIN; PARKER HSING-YEH
权利人:MICROSOFT TECHNOLOGY LICENSING LLC
摘要:High surface area coatings are applied to solid substrates to increase the surface area available for solid-phase synthesis of polymers. The high surface area coatings use three-dimensional space to provide more area for functional groups to bind polymers than an untreated solid substrate. The polymers may be oligonucleotides, polypeptides, or another type of polymer. The solid substrate is a rigid supportive layer made from a material such as glass, a silicon material, a metal material, and plastic. The coating may be thin films, hydrogels, microparticles. The coating may be made from a metal oxide, a high-κ dielectric, a low-κ dielectric, an etched metal, a carbon material, or an organic polymer. The functional groups may be hydroxyl groups, amine groups, thiolate groups, alkenes, n-alkenes, alkalines, N-Hydroxysuccinimide (NHS)-activated esters, polyaniline, aminosilane groups, silanized oxides, oligothiophenes, and diazonium compounds. Techniques for applying coatings to solid substrates and attaching functional groups are also disclosed.

专利号:US-8653282-B2
优先权日:2007-10-18
标 题:Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein
发明人：FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G
权利人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G; BOEHRINGER INGELHEIM INT
摘要:The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO 2 , preferably SO, and wherein R A , R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.

专利号:US-7858808-B2
优先权日:2002-05-31
标 题:Multi-substituted imidazolines and method of use thereof
发明人：TEPE JETZE J; PEDDIBHOTLA SATYAMAHESHWAR
权利人:UNIV MICHIGAN STATE
摘要:A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 μm/mL.