专利号:WO-2020248279-A1 优先权日:2019-06-14 标 题 :Continuous synthesis method for substituted benzoate organic matter 发明人:HONG HAO; LU JIANGPING; ZHANG ENXUAN; LIU ZHIQING; LI CHAO 权利人:JINLIN ASYMCHEM LABORATORIES CO LTD 摘要:The present invention provides a continuous synthesis method for a substituted benzoate organic matter. The continuous synthesis method comprises: in the presence of a catalyst and an organic solvent, continuously feeding an organic matter as represented by formula (I) and oxygen into a continuous reaction device for continuous oxidation reaction to obtain a substituted benzoate organic matter, and performing continuous discharge, wherein the substituted benzoate organic matter has a structure as represented by formula (II). Oxygen is a green reagent, and is cheap and easy to obtain; the present invention would not produce a large amount of waste gas, waste water, and waste residues after the completion of reaction, and the system is easy to handle. The use of continuous reaction operation can reduce the risk of solvent flash evaporation explosion due to high concentration oxygen in batch reactions. Under the same oxidation conditions, the use of a continuous preparation process can reduce the escape of oxygen, greatly increase the utilization of oxygen, simplify the operation, and improve the reaction safety and the yield of substituted benzoate organic matters.
专利号:US-8350100-B2 优先权日:2002-03-15 标题 :Process for the preparation of ring compounds 发明人:PAULUTH DETLEF; KIRSCH PEER; BAEUERLE PETER; DEEG OLIVER 权利人:MERCK PATENT GMBH; PAULUTH DETLEF; KIRSCH PEER; BAEUERLE PETER; DEEG OLIVER 摘要:In a process for the preparation of ring compounds via a combinatorial synthesis, the reaction procedure is based on a Suzuki coupling; subsequent halo-demetallation and finally a further Suzuki coupling. The Suzuki couplings are each carried out with a boronic acid or a boronic acid ester. The reaction procedure uses provides novel ring compounds and uses novel synthesis units used for this purpose. The novel ring compounds are suitable for use as constituents in liquid-crystalline mixtures.
专利号:US-9012445-B2 优先权日:2012-01-12 标题 :Substituted 4-(1H-pyrazol-4-yl)benzyl analogues as positive allosteric modulators of mAChR M1 receptors 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; POSLUSNEY MICHAEL S; TARR JAMES C 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-5922866-A 优先权日:1995-08-30 标题:Process for preparing quinazolin-4-one derivatives 发明人:MIYATA KAZUYOSHI; KUROGI YASUHISA; SAKAI YASUHIRO; TSUDA YOSHIHIKO 权利人:OTSUKA PHARMA CO LTD 摘要:The present invention provides a novel process for preparing a series of quinazolin-4-one derivatives in high yields with reduced amounts of byproducts, the process comprising reacting, in the presence of a base, a trialkylsilyl halide with a compound represented by the formula ##STR1## wherein; R 5 is a phenyl group which may have 1 to 3 substituents each selected from a lower alkyl group, a lower alkoxy group or a halogen atom, a lower alkyl group, a phenyl-lower alkyl group which may have a halogen atom as a substituent on the phenyl ring, a lower alkenyl group, a lower alkoxy-lower alkyl group or a lower alkynyl group; R 6 is a lower alkyl group, a halogen-substituted lower alkyl group, a lower alkoxycarbonyl group or a phenyl group which may have, as a substituent, a lower alkyl group or a group of the formula ##STR2## wherein A is an oxygen atom or a single bond, Z is a lower alkylene group, R 7 is a lower alkyl group and R 8 is a lower alkoxy group, a phenyl group or a phenyl-lower alkoxy group which may have a halogen atom on the phenyl ring; n to produce the quinazolin-4-one derivatives which is valuable as pharmaceuticals or intermediates for synthesis thereof and represented by the formula ##STR3## wherein R 1 ,R 2 , R 3 , R 4 , R 5 , and R 6 are as defined above.
专利号:JP-H10502532-A 优先权日:1994-07-08 标 题:Novel streptogramins and methods for the production of streptogramins by muta synthesis
专利号:CN-115087647-A 优先权日:2018-12-07 标 题:For the preparation of 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl) ) ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine synthesis method