专利号:US-5567830-A 优先权日:1994-02-14 标题 :Process for synthesis of acetylenic carbinols 发明人:UPASANI RAVINDRA B 权利人:COCENSYS INC 摘要:A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
专利号:US-5449795-A 优先权日:1994-02-14 标 题 :Process for synthesis of steroidal allylic tert. alcohols 发明人:HOGENKAMP DERK J 权利人:COCENSYS INC 摘要:A method for the preparation of a steroidal allylic tertiary alcohol is disclosed which involves the deprotonation of a sulfoxide with a strong base which is capable of deprotonating the methine proton which is α to the sulfoxide, in an inert solvent to give the anion; reaction of the anion with a steroidal spiro-2'-oxirane to give a steroidal γ-hydroxysulfoxide; and thermolysis in the presence of a base other than calcium carbonate to give the steroidal allylic tertiary alcohol.
专利号:US-3555015-A 优先权日:1968-09-17 标 题 :Process for the preparation of gona-1,3,5(10),7-tetraenes 发明人:STEIN REINHARDT P; BUZEY GEORGE C JR; SMITH HERCHEL 权利人:AMERICAN HOME PROD 摘要:TREATMENT OF A 13-ALKYLGONA-1,3,5(10),8-TETRAENE WITH ORGANIC PERACID RESULTS IN THE FORMATION OF A CORRESPONDING 8,9-EPOXY-13-ALKYLGONA-1,3,5(10)-TRIENE, WHICH UPON TREATMENT WITH ACID, IS RING-OPENED AND REARRANGED TO THE CORRESPONDING 13-ALKYLGONA-1,3,5(10),9(11)-TETRAEN-8-OL. CATALYTIC HYDROGENATION THEN AFFORDS THE CORRESPONDING 13-ALKYLGONA-1,3,5(10)-TRIEN-8-OL WHICH UPON DEHYDRATION GIVES THE CORRESPONDING 13-ALKYLGONA-1,3,5(10),7-TETRAENE. THERE IS THUS PROVIDED A ROUTE TO THE SYNTHESIS OF EQUILIN AND RELATED COMPOUNDS.
专利号:US-7105637-B2 优先权日:2002-02-15 标题 :Dehydro-estriol (8-DHE3) and dehydro-pregnanetriol (7-DHPT), methods of their synthesis 发明人:SHACKLETON CEDRIC; GUO LI-WEI; WILSON WILLIAM K 权利人:CHILDRENS HOSP & RES CT OAK 摘要:The invention provides isolated dehydro-estriol (8-DHE 3 ) and dehydro-pregnanetriol (7-DHPT), and methods of their synthesis. These compounds are useful in diagnosis of Smith-Lemli-Optiz syndrome (SLOS).
专利号:US-2013261317-A1 优先权日:2010-09-27 标题 :Methods for preparing synthetic bile acids and compositions comprising the same 发明人:MORIARTY ROBERT M; RAO PHOTON 权利人:MORIARTY ROBERT M; RAO PHOTON; KYTHERA BIOPHARMACEUTICALS INC 摘要:This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C 14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.
专利号:EP-0354945-B1 优先权日:1988-01-13 标 题 :Process for the enhancement of enzyme activities and synthetic efficiency in microorganisms and higher plants 发明人:FIEDLER FRANZ; ZENK MEINHART H; GUNDLACH HEIDRUN; WEBER ALFRED; KENNECKE MARIO 权利人:SCHERING AG 摘要:In the process disclosed, the organisms are brought into contact witn inactivated elicitor-containing microorganisms, fragments of the latter, or excretions of elicitor-containing microorganisms. Only inactivated elicitor-containing bacteria, fragments of the latter, or excretions of elicitor-containing bacteria may be used to activate enzymes and promote synthesis in non-microbial organisms. The process can be used, for example, to promote synthesis in microorganisms or plants which produce pigments, antibiotics, alkaloids or phytoalexins or to activate enzymes in microorganisms capable of transforming steroids.
摘要:Hitomi, Y.; Arakawa, K., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 297. 摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 参考文献:10.1016/s0304-3940(02)00146-5 摘要:Rozovsky I, Hoving S, Anderson CP, O'Callaghan J, Finch CE. Equine estrogens induce apolipoprotein E and glial fibrillary acidic protein in mixed glial cultures. Neurosci Lett. 2002 May 03;323(3):191–4. doi: 10.1016/s0304-3940(02)00146-5. 参考文献:10.1016/s1071-5576(01)00111-3|10.1177/107155760100800410 摘要:Berco M, Bhavnani BR. Differential Neuroprotective Effects of Equine Estrogens Against Oxidized Low Density Lipoprotein—Induced Neuronal Cell Death. Journal of the Society for Gynecologic Investigation. 2001 Jul;8(4):245–54. doi: 10.1177/107155760100800410. 摘要:Mayer P, Tse S, Sendi M, Bourg D, Morrison D. Steady-state pharmacokinetics of conjugated equine estrogens in healthy, postmenopausal women. J Reprod Med. 2008 Feb;53(2):97–101.