专利号:US-11542269-B2 优先权日:2018-01-03 标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHOI HYEONG-WOOK; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-11136335-B2 优先权日:2016-06-30 标题:Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHASE CHARLES E; CHOI HYEONG-WOOK; ENDO ATSUSHI; FANG FRANCIS G; KIM DAE-SHIK 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
专利号:US-5760249-A 优先权日:1995-08-29 标题 :Synthesis of hydroxysulfone and related compounds 发明人:MATHRE DAVID J; SOHAR PAUL; MOODY DAVID; BLACKER ANDREW J 权利人:MERCK & CO INC; ZENECA LTD 摘要:This invention is concerned with an improved process for the synthesis of hydroxysulfone, which is a key intermediate in the synthesis of carbonic anhydrase inhibitors, especially dorzolamide. Carbonic anhydrase inhibitors are known to be effective in treating elevated intraocular pressure or glaucoma.
专利号:US-RE37449-E 优先权日:1987-02-06 标题:Process of synthesis of 3′,4′-anhydrovinblastine, vinblastine and vincristine 发明人:KUTNEY JAMES P; CHOI LEWIS S L; NAKANO JUN; TSUKAMOTO HIROKI; BOULET CAMILLE A; MCHUGH MICHAEL 权利人:UNIV BRITISH COLUMBIA 摘要:The present invention relates to the synthesis of dimer alkaloid compounds, particularly those of the Catharantus (Vinca) family, from an indole unit, such as cantharanthine, and a dihydroindole unit, such as vindoline. A multi-step process is disclosed including the steps of (1) of 1,4-reduction of a first dimeric iminium intermediate to an enamine compound by reaction with a 1,4-dihydropyridine compound; (2) oxidative transformation of the resulting enamine to a second iminium intermediate under controlled aeration; (3) reduction of the second iminium intermediate to form the target dimer alkaloid compounds. The entire process can be conducted in a one-pot operation to obtain the target compounds without isolation of the intermediates.
专利号:EP-0853625-B1 优先权日:1995-08-29 标 题:Synthesis of hydroxysulfone and related compounds 发明人:MATHRE DAVID J; SOHAR PAUL; MOODY DAVID; BLACKER ANDREW J 权利人:MERCK & CO INC; SYNGENTA LTD 摘要:This invention is concerned with an improved process for the synthesis of hydroxysulfone, which is a key intermediate in the synthesis of carbonic anhydrase inhibitors, especially dorzolamide. Carbonic anhydrase inhibitors are known to be effective in treating elevated intraocular pressure or glaucoma.
专利号:US-10981922-B2 优先权日:2012-04-26 标题 :Synthesis of lactams 发明人:TAVARES FRANCIS XAVIER 权利人:TAVARES FRANCIS XAVIER 摘要:Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC—OR—NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam.
参考标题:Synthesis Of Aromatic Aldehydes Via 2-Aryl-N,N'-Diacyl-4-Imidazolines 作者:Jan Bergman,Lars Renström,Birger Sjöberg |发布日期:1980.1 摘要:Diacylimidazolium Ions Yield Adducts With Aromatic Compounds. Thus The N,N'-Diacetylimidazolium Ion And Indole Gives 1,3-Diacetyl-2-(3-Indolyl)-4-Imidazoline. Less Reactive Substrates Such As Thiophene, Anisole And 1,3-Dimethylbenzene Fail To React With This Reagent But Do Form Adducts (E.G. 1,3-Bis-(Trifluoroacetyl)-2-(2-Thienyl)-4-Imidazoline) With An Imidazole/trifluoroacetic Anhydride Reagent.
合成参考文献
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