专利号:US-11390590-B2 优先权日:2016-08-16 标 题 :Methods and processes for the preparation of KDM1A inhibitors 发明人:TAPPER AMY E; CELATKA CASSANDRA; ROMERO ARTHUR GLENN; MCCALL JOHN M; CHANCELLOR TONI; CHEN JIAN-XIE; CHEN XUEMEI; ZHAO HE; BIOLATTO BETINA; BROT ELISABETH C A; LI ZHIHUA; LIAO XIAOMING 权利人:IMAGO BIOSCIENCES INC 摘要:Provided in this disclosure are methods for the synthesis of substituted 2-arylcyclopropylamines and 2-heteroarylcyclopropylamines and related compounds. Also provided are methods for reduction of thioesters to aldehydes, and methods for reductive animation of cyclopropylamines.
专利号:US-2021171437-A1 优先权日:2017-07-17 标题 :Peptide nucleic acid (pna) monomers with an orthogonally protected ester moiety and novel intermediates and methods related thereto 发明人:COULL JAMES M; GILDEA BRIAN D 权利人:VERA THERAPEUTICS INC 摘要:The present disclosure pertains to peptide nucleic acid (PNA) monomers and oligomers, as well as methods and compositions useful for the preparation of PNA monomer precursors (e.g. PNA Monomer Esters, Backbone Esters and Backbone Ester Acid Salts, as described below) that can be used to prepare PNA monomers wherein said PNA monomers can be used to prepare said PNA oligomers. In some embodiments, the disclosure features sulfonic acid salts of Backbone Ester compounds, which sulfonic acid salts generally tend to be crystalline and can be obtained in reasonably good yield, often without requiring any chromatographic purification of the reaction product of the Backbone Ester synthesis reaction. This disclosure also pertains to novel methods for the synthesis of said Backbone Ester compounds and novel methods for the formation of the related sulfonic acid salts. Exemplary ester groups include, but are not limited to, 2,2,2-trichloroethy-(TCE), 2,2,2-tribromoethyl-(TBE), 2-iodoethyl-groups (2-IE) and 2-bromoethyl-(2-BrE) as the ester group. These particular ester groups can be removed under conditions where both Boc and Fmoc protected amine groups are stable.
专利号:US-9254298-B2 优先权日:2008-07-31 标 题 :Synthesis and formulations of salts of isophosphoramide mustard and analogs thereof 发明人:WALIGORA FRANK W; AMEDIO JR JOHN C 权利人:ZIOPHARM ONCOLOGY INC 摘要:Disclosed herein are formulations and methods of manufacture of compounds of formula (E): n nwherein X and Y independently represent leaving groups; and A + is an ammonium cation.
专利号:US-2022185846-A1 优先权日:2019-03-28 标 题:Methods for synthesizing beta-homoamino acids 发明人:MANTHATI SURESH KUMAR; BHANDARI ASHOK; MASJEDIZADEH MOHAMMAD REZA 权利人:PROTAGONIST THERAPEUTICS INC 摘要:Methods of making β-homoamino acids as intermediate for synthesis of peptide monmer and dimer α4β7-antagonists are disclosed. The disclosed methods include solid phase and solution phase methods.
专利号:CN-115925790-A 优先权日:2016-03-23 标 题:Method for the synthesis of α4β7 peptide antagonists
专利号:ES-2987575-T3 优先权日:2015-08-12 标 题:Intermediates for the synthesis of microbicidal heterobicyclic derivatives
[参考文献]: Jean-Damien Charrier, Et Al. Synthesis Of (2S,4S)- And (2S,4R)-5-Fluoroleucine And (2S,4S)-[5,5-2H2]-5-Fluoroleucine. Org Biomol Chem. 2004 Feb 21;2(4):474-82.
合成参考文献
参考文献:10.1055/s-2006-955670 摘要:Shi Y, Shen Y-, Zhao M-, Xu J. Aziridination of Chalcones Using Tertiary Amine Catalysts. Synfacts. 2007 Jan;2007(1):0101. doi: 10.1055/s-2006-955670.