专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-2007149782-A1 优先权日:2005-12-23 标 题:Methods of preparing a crystalline form of 7-(4-chlorobutoxy)-3,4-dihydro-2(1h)-quinolinone and the use thereof in the synthesis of Aripiprazole 发明人:BRAND MICHAEL; SHOOKRUN MOTY; GRIBUN IRINA; ADIN ITAI; IUSTAIN CARMEN; BRAVERMAN OLEG; UDIS NATALIA; ARAD ODED; KASPI JOSEPH 权利人:BRAND MICHAEL; SHOOKRUN MOTY; GRIBUN IRINA; ADIN ITAI; IUSTAIN CARMEN; BRAVERMAN OLEG; UDIS NATALIA; ARAD ODED; KASPI JOSEPH 摘要:The present invention relates to methods of preparing a highly pure crystalline form of 7-(4-chlorobutoxy)-3,4-dihydro-2(1H)-quinolinone, which is a chemical intermediate useful in the preparation of Aripiprazole thereof in high quality and yield, and provides data that characterizes the crystalline form of 7-(4-chlorobutoxy)-3,4-dihydro-(1H)-quinolinone.
专利号:WO-2022190047-A1 优先权日:2021-03-12 标题:Process for consecutive continuous-flow reductions in the synthesis of medicinally relevant piperazine derivatives using a tubular reactor with alternating diameter 发明人:BANA PÉTER; FÜLÖP ZSOLT; ÉLES JÃ?NOS 权利人:RICHTER GEDEON NYRT 摘要:The present invention relates to a novel alternating diameter flow reactor for continuous - flow reactions, a system for continuous-flow reactions (as shown in Figure 1) comprising said alternating diameter flow reactor, a method for the formation of the C-N bond carried out in said system and a process for the preparation of the antipsychotic drug cariprazine described by the chemical structure (I) and its intermediates, and as well as other related 1-arylpiperazine active pharmaceutical ingredients conducted in two continuous-flow reactors of said system comprising the consecutive steps of a first step being selective ester reduction carried out in said alternating diameter flow reactor and a second step being reductive amination carried out by continuous-flow catalytic hydrogenation.
专利号:US-2024215280-A1 优先权日:2022-10-31 标 题:In situ core/shell perovskite nanocrystal material, method of preparation thereof, and light emitting device comprising the same 发明人:LEE TAE-WOO; KIM JOO SUNG 权利人:SEOUL NAT UNIV R&DB FOUNDATION; PEROLED CO LTD 摘要:The present inventive concept relates to an in situ core/shell perovskite nanocrystal film formed by an in situ nanocrystal synthesis process, a method for producing the same, and a light emitting device comprising the same as a light-emitting layer. The in situ core/shell perovskite nanocrystal film formed by the in situ nanocrystal synthesis process according to the present inventive concept exhibits a strong charge confinement effect by nanocrystal formation, and can simultaneously greatly improve the luminescence efficiency and lifetime by maintaining the fast charge transport capability of polycrystalline perovskite.
专利号:US-4806601-A 优先权日:1984-11-08 标 题:Polyarylene polyethers with pendant vinyl and ethynyl groups and process for preparation thereof 发明人:PERCEC VIRGIL 权利人:GOODRICH CO B F 摘要:A method for the synthesis of polyarylene polyether (PAPE) oligomers with pendant vinyl groups is presented. Aromatic polyether sulfone (APS) and poly(2,6-dimethyl-1,4-phenylene oxide) (PPO) backbones are used for specific examples. Terminal vinyl groups may also be provided on the APS by forming the alpha , omega -di(benzyl)APS before the first step of a synthesis to form a pendant groups which step involves the chloromethylation of APS and PPO to provide oligomers with chloromethyl groups. PPO containing bromomethyl groups was obtained by radical bromination of the PPO methyl groups. Both chloromethylated and bromomethylated starting materials are converted to their phosphonium salts, and then subjected to a phase transfer catalyzed Wittig reaction to provide the pendant vinyl groups. An APS containing pendant ethynyl groups is prepared by bromination of the APS with pendant vinyl groups, followed by a phase transfer catalyzed dehydrobromination. Differential scanning calorimetry analysis of the thermal curing of the oligomers containing pendant vinyl groups, and, ethynyl groups, showed that the curing reaction is much faster for the former. The resulting network polymers were flexible when the starting oligomer contained pendant vinyl groups, and very rigid when it contained pendant ethynyl groups.
专利号:US-9718795-B2 优先权日:2013-10-14 标题:1,4-cyclohexylamine derivatives and processes for the preparation thereof 发明人:TADDEI MAURIZIO; CINI ELENA; RASPARINI MARCELLO 权利人:CHEMO RES S L 摘要:The invention relates to a process for the synthesis of Cariprazine, an antipsychotic compound useful in the treatment of positive and negative symptoms associated to schizophrenia, with the following structural formula: (A) The invention further relates to the synthesis of intermediates useful in the preparation of Cariprazine.