专利号:US-4240961-A 优先权日:1979-05-29 标 题 :Synthesis of 2-piperazinones and 1,4-diaza-2-keto-cycloheptanes 发明人:LAI JOHN T 权利人:GOODRICH CO B F 摘要:Substituted 2-piperazinones are prepared by reacting a substituted 1,2-diamine with (a) an acyclic or cyclic cyanohydrin acetate, (b) a haloform, and (c) alkali metal hydroxide, in the presence of a suitable organic solvent, at ambient pressure and temperature preferably lower than about 20° C. In an analogous manner, substituted 1,4-diaza-2-keto-cycloheptanes are prepared by reacting substituted 1,3-propane-diamines. In this synthesis, referred to as 'the cyanohydrin acetate synthesis,' the reaction is accelerated with a phase transfer catalyst selected from the group consisting of a polyether, an onium salt, and a tertiary amine. This synthesis yields predominantly a 2-keto-diazacycloalkane with substituents desirably substituted on carbon atoms on either side of the N 4 atom of the diaza ring.
专利号:US-4246412-A 优先权日:1979-08-27 标 题:Synthesis of 2-keto-1,4-diazacycloalkanes with a soft ion catalyst 发明人:LAI JOHN T 权利人:GOODRICH CO B F 摘要:A phase transfer catalyzed 'soft ion synthesis' is disclosed in which the presence of a 'soft ion' generated in situ by a soft ion catalyst has a directive effect which favors the formation of a polysubstituted 2-keto-1,4-diazacycloalkane isomer having substituents on both N4-adjacent carbon atoms ('C atoms') of its diaza ring; this isomer is formed at the expense of isomers in which an N4-adjacent C atom is not substituted. Such an isomer which has substituents on each N4-adjacent C atom is generally more effective as a u-v light stabilizer than an isomer which has an unsubstituted N4-adjacent C atom, and therefore the former is more desirable. A liquid phase reaction of an acyclic 1,2-diamine with a monoketone or monoaldehyde in the presence of a phase transfer catalyst, a haloform and alkali is disclosed, in which reaction a soft ion catalyst which generates a soft ion selected from the group consisting of cyanide, iodide and thiocyanate, has a directive effect on the reaction so as to produce more isomer with substituents on each N4-adjacent C atom than would be formed, under identical conditions but without the presence of the soft ion. The directive effect of the soft ion appears to enhance any directive effect that a particular phase transfer catalyst may exhibit.
专利号:US-4711957-A 优先权日:1979-07-13 标题 :Synthesis of 2-keto-1,4-diazacycloalkanes 发明人:LAI JOHN T 权利人:GOODRICH CO B F 摘要:The disclosure deals with novel synthesis involving (a) hydrogenation of a cis-3,3-dialkyl-3,4-dihydroquinoxaline-2-one in the presence of a suitable hydrogenation catalyst, at elevated temperature and pressure, to yield a cis-3,3-dialkyl decahydroquinoxaline-2-one; (b) reaction of trans-1,2-diaminocyclohexane with acetone cyanohydrin in the presence of water to yield trans-3,3-dimethyl-decahydroquinoxaline-2-one; and (c) a reaction of 1,2-diamine with a saturated acyclic or cyclic monoketone or aldehyde and a holoform, in the presence of (i) a phase transfer catalyst (ii) an organic solvent, and (iii) solid or aqueous alkali to yield 2-keto-1,4-diazacycloalkanes. Such compounds exhibit exceptional UV light stabilizing property.
专利号:EP-0468457-B1 优先权日:1990-07-24 标题 :Novel substituted piperidines and their use as inhibitors of cholesterol synthesis 发明人:MCCARTHY JAMES R; BARNEY CHARLOTTE L; WANNAMAKER MARION W 权利人:MERRELL DOW PHARMA 摘要:The present invention relates to a group of compounds which are novel substituted piperidines and which act to inhibit the synthesis of cholesterol in mammals and in fungi.
专利号:US-2023219881-A1 优先权日:2022-01-11 标题 :Synthesis of Spermidine, Spermine, and Free Bases Thereof 发明人:TITLOW MATTHEW; GU XINGLONG 权利人:COMPOUND SOLUTIONS INC; SHAOXING KING YEAR BIOCHEMICAL CO LTD 摘要:A simplified synthetic process for production of spermine and spermidine are presented that can provide spermine and spermidine in free base or salt form. Advantageously, the synthetic procedure is safe, simple, and environmentally friendly, while at the same time also being cost-effective.
专利号:US-4219684-A 优先权日:1979-04-02 标 题 :Synthesis of alcohols by hydroformylation with nitrile promoter 发明人:IMAI TAMOTSU 权利人:UOP INC 摘要:Alcohols may be synthesized by reacting an olefinic compound, carbon monoxide and hydrogen in the presence of a Group VIII organometallic complex catalyst at reaction conditions which include a temperature in the range of from about 50° to about 250° C. and a pressure in the range of from about 10 to about 300 atmospheres. In addition, the reaction is also effected in the presence of a promoter compound comprising a nitrile.
[参考文献]: Mustafa Z Zel, Et Al. New Sensitive And Quantitative Analysis Method For Organic Nitrogen Compounds In Urban Aerosol Samples. Environ Sci Technol. 2011 Feb 15;45(4):1497-505.
合成参考文献
摘要:Shimizu, T., Science of Synthesis Knowledge Updates, (2011) 1, 494. 摘要:Tauchert, M. E., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 1, 332. 摘要:Archives of Toxicology., 55(47), 1984 [] 摘要:Adak, L.; Sahoo, S.; Aoki, S.; Kawanaka, Y.; Nakamura, M., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 408.