专利号:US-8598346-B2 优先权日:2008-07-16 标 题 :Synthesis of cyclic amidines 发明人:LENTZEN GEORG; NEUHAUS THORSTEN 权利人:LENTZEN GEORG; NEUHAUS THORSTEN; BITOP AG 摘要:The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a β-, γ- or δ-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.
专利号:US-4190579-A 优先权日:1977-12-29 标题:Synthesis of beta-lactams from azetidine carboxylic acid esters 发明人:LIPSHUTZ BRUCE H; WASSERMAN HARRY H; WU JAMES S 权利人:RESEARCH CORP 摘要:Azetidine carboxylic acid esters are converted into enol silyl ethers which, as enamino ketene acetals, undergo ready oxidative cleavage of the ethylenically unsaturated double bond, e.g. by dye-sensitized photo-oxygenation, to form beta-lactams. The beta-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams.
专利号:US-4442298-A 优先权日:1982-08-30 标 题:Chemical synthesis of ethylene/maleic anhydride dimer with phenylethyl end group 发明人:TOU JACOB S; SCHLEPPNIK ALFRED A 权利人:MONSANTO CO 摘要:A phenylethyl substituted dimer of ethylene and maleic anhydride, names 7-phenyloctane-(1,2),(5,6)-dianhydride, is chemically synthesized by n (a) alkylating alkyl 2,4-dihalobutyrate with alkyl 2-cyano-3-phenylbutyrate, n (b) alkylating the resulting halide condensation product with a carboxylate selected from the group consisting of trialkyl ethane-1,1,2-tricarboxylate and dimethyl cyanoethane-1,2-dicarboxylate, n (c) acid hydrolyzing the resulting tetra or pentaester accompanied by decarboxylating, and n (d) dehydrating the resulting tetra-acid to yield the desired phenylethyl substituted dimer of ethylene and maleic anhydride, n wherein the alkyls in the butyrate and carboxylate ester groups each contain from one to about four carbon atoms and halo is selected from the group consisting of bromo, chloro and iodo. n The dimer has anti-tumor and anti-viral properties and can be used in silver halide emulsions.
专利号:US-4234744-A 优先权日:1978-12-18 标 题 :Process for the production of aminoacid hydrochlorides/or diaminoacid dihydrochlorides 发明人:EFFENBERGER FRANZ; DRAUZ KARLHEINZ 权利人:DEGUSSA 摘要:Aminoacid hydrochlorides or diaminoacid dihydrochlorides are produced by first reacting a halocarboxylic acid ester with an alkali metal cyanate in the presence of an alcohol to form the corresponding mono- or diurethane and then saponifying this to the corresponding mono- or dihydrochloride. The new process is relatively versatile in its use and above all opens up an elegant synthesis route for lysine.
专利号:US-9751874-B2 优先权日:2014-12-17 标题:Hydroxy containing FXR (NR1H4) modulating compounds 发明人:GEGE CHRISTIAN; KINZEL OLAF; KREMOSER CLAUS; SCHMITT AARON C 权利人:GILEAD SCIENCES INC 摘要:The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:WO-2025123046-A1 优先权日:2023-12-07 标 题:Synthesis of leucine-rich repeat kinase 2 modulators 发明人:STORZ THOMAS; DONG HANQING; CHEN CHUNGPIN HERMAN 权利人:ARVINAS OPERATIONS INC 摘要:Provided are methods for synthesizing compounds having activity against Leucine- rich repeat kinase 2 (LRRK2), as well as intermediates generated during said methods.
参考标题:Synthesis Of Cyclic Amidines 摘要:The Invention Relates To An Innovative Method For Synthesis Of Cyclic Amidines. The Synthesis Starts From A β-, γ- Or δ-Lactone Which Is Twofold Brominated. After Esterification Of The Carboxyl Function, The Bromine Atoms Are Nucleophilically Substituted And The Corresponding Diamino Compound Is Obtained. The Ring Closure To The Cyclic Amidine Is Accomplished Subsequently By Reaction With Orthoester, Imidate Or Thioimidate. Owing To Interposing Additional Steps For Recovery Of The Diamino Compound In Enantiomerically Pure Form, The Enantiomers Of The Cyclic Amidines Can Be Stereoselectively Synthesized.
合成参考文献
参考文献:10.1055/s-0040-1720323 摘要:Synthesis of Ceralasertib. Synfacts. 2021 Mar 18;17(04):0371. doi: 10.1055/s-0040-1720323. 参考文献:10.1055/s-0033-1340822 摘要:Compain P. Searching for Glycomimetics That Target Protein Misfolding in Rare Diseases: Successes, Failures, and Unexpected Progress Made in Organic Synthesis. Synlett. 2014 Mar 14;25(09):1215–40. doi: 10.1055/s-0033-1340822.