专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:EP-1735276-B1 优先权日:2004-04-02 标题:Novel method for the preparation of intermediates useful for the synthesis of vitamin d analogues 发明人:HANSEN ERIK TORNGAARD; SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; PEDERSEN HENRIK; DEUSSEN HEINZ-JOSEF WILHELM 权利人:LEO PHARMA AS 摘要:The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.
专利号:EP-3617181-A1 优先权日:2018-08-30 标题:Synthesis of trans-2-phenylcyclopropylamine or a salt or solvate thereof 发明人:BREUNING ALEXANDER; LIMMERT MICHAEL; DELLING AXEL; HOFMEIER HARALD; HULTSCH JANA; MICKSCH MAIK; SOMMER CHRISTIAN 权利人:AREVIPHARMA GMBH 摘要:The present invention relates to the field of manufacturing trans-2-phenylcyclopropylamine or a salt or solvate thereof, in particular in the form of the sulphate salt. The obtained product, particularly when in the form of the synthesis of trans-2-phenylcyclopropylamine sulphate, is exceptionally pure, substantially free from reactants and reagents that are mutagenic, hazardous or of great concern to the health of humans or the environment.
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
专利号:US-2024309003-A1 优先权日:2021-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
摘要:Molander, G. A.; Beaumard, F., Science of Synthesis Knowledge Updates, (2013) 3, 128. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 355. 摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 77. 摘要:Margaretha, P., Science of Synthesis Knowledge Updates, (2010) 1, 117. 摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 74.