丙二酸环(亚)异丙酯,原甲酸三乙酯 以54%的收率获得5-(甲氧基甲烯基)-2,2-二甲基-1,3-二氧己环-4,6-二酮 参考文献:Strategic Studies In The Syntheses Of Novel 6,7-Substituted Quinolones And 7-Or 6-Substituted 1,6-And 1,7-Naphthyridones 标题:Strategic Studies In The Syntheses Of Novel 6,7-Substituted Quinolones And 7-Or 6-Substituted 1,6-And 1,7-Naphthyridones 摘要:This Paper Describes The Different Strategies Devised And Applied To Overcome The Selectivity Issues In The Syntheses Of 6,7-Disubstituted-1H-Quinolin-4-One,7-Substituted-1H-1,6-Naphthyridin-4-One And 6-Substituted-1H-1,7-Naphthyridin-4-One Derivatives. They Allowed Us To Improve The Overall Yields And The Scating-Up Feasibility. Several Examples Illustrate These Strategies With Their Advantages And Drawbacks. (C) 2008 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tet.2008.01.055
专利号:EP-0310849-B1 优先权日:1987-10-05 标题:Process for the synthesis of a benzo [ij] quinolizine-2-carboxylic acid derivative 摘要:Process for preparing 6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carbo xylic acid (flumequine, I) wherein 6-fluoro-2-methyl-1,2,3,4-tetrahydroquinoline (II) is reacted in the presence of a catalyst with an alkyl ortho-formate (IX), wherein R3 represents a C1-C4 alkyl, and with a 2,2-disubstituted 1,3-dioxan-4,6-dione, wherein each R1 and R2, which can be the same or different, represents a hydrogen atom, a branched- or straight-chain C1-C6 alkyl or phenyl, or R1 and R2 together represent a polymethylene group -(CH2)n-, n= 4 or 5, so as to form a 2,2-disubstituted 5- [1-(6-fluoro-2-methyl-1,2,3,4-tetrahydroquinolyl)] methylene-1,3-dioxan -4,6-dione of formula (VII): and then said compound of formula (VII) is reacted in the presence of polyphosphoric acid and ethyl polyphosphate, whereby the desired compound (I) is directly obtained and isolated according to conventional methods.
专利号:EP-0310849-A1 优先权日:1987-10-05 标题 :Process for the synthesis of a benzo [ij] quinolizine-2-carboxylic acid derivative
专利号:WO-2024038357-A1 优先权日:2022-08-16 标 题:Synthesis of substituted tetracyclic carboxylic acids and analogues thereof 发明人:CHEN SHUAI; COLE ANDREW G; GOTCHEV DIMITAR B; MASON JEREMY; PALLERLA MAHESH KUMAR; PAMULAPATI GANAPATI REDDY; SPINK JAN MICHELLE 权利人:ARBUTUS BIOPHARMA CORP 摘要:The present disclosure includes synthetic methods for preparing certain substituted tetracyclic carboxylic acids, which can be used to treat, ameliorate, or prevent hepatitis B virus (HBV) infections in a patient.