专利号:US-4310467-A 优先权日:1980-10-22 标题:Process and intermediates for the synthesis of vitamin D3 metabolites 发明人:BATCHO ANDREW D; BERGER JR DONALD E; USKOKOVIC MILAN R 权利人:HOFFMANN LA ROCHE 摘要:The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D 3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 20-position. These novel intermediates are prepared from 17-keto steroids by reaction with ethyltriphenylphosphonium halides followed by reaction with formaldehyde to form comounds having the natural steroid configuration at the 20-position and which are suitable substrates for the preparation of the aforementioned Vitamin D 3 metabolites.
专利号:US-11826833-B2 优先权日:2013-04-12 标 题 :Synthesis of bimetallic nanoparticle catalysts using microwave irradiation 发明人:HUMPHREY SIMON M; GARCIA STEPHANY 权利人:UNIV TEXAS 摘要:The present invention provides compositions and methods of making bimetallic metal alloys of composition for example, Rh/Pd; Rh/Pt; Rh/Ag; Rh/Au; Rh/Ru; Rh/Co; Rh/Ir; Rh/Ni; Ir/Pd; Ir/Pt; Ir/Ag; Ir/Au; Pd/Ni; Pd/Pt; Pd/Ag; Pd/Au; Pt/Ni; Pt/Ag; Pt/Au; Ni/Ag; Ni/Au; or Ag/Au prepared using microwave irradiation.
专利号:US-4360684-A 优先权日:1981-04-08 标 题 :Process for the preparation of (2S)-tetrahydro-2α-methyl-6-oxo-4βα-carboxylic acid 发明人:CVETOVICH RAYMOND J; MELILLO DAVID G; RYAN KENNETH M; SLETZINGER MEYER 权利人:MERCK & CO INC 摘要:Disclosed is a process for preparing (2S)-tetrahydro-2 alpha -methyl-6-oxo-4 beta -amino-2H-pyran-3 alpha -carboxylic acid (I) which is useful in the synthesis of thienamycin. The process proceeds via a stereospecific reduction of the 2-acetyl-3-(R)- alpha -methylbenzylamino-2-pentenedioic acid diester (II). I II wherein R is, alpha -methylbenzyl, and R1 is lower alkyl having 1-6 carbon atoms or arylalkyl such as benzyl.
专利号:US-2025282777-A1 优先权日:2024-03-06 标 题:Methods of Making Tolebrutinib 发明人:BALTES DAVID; BOHORC BOJAN; SAKHAII PEYMAN 权利人:PRINCIPIA BIOPHARMA INC 摘要:Disclosed herein are improved synthetic routes for making (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1H-imidazo[4,5-c]pyridin-2(3H)-one (tolebrutinib). Also disclosed herein are novel compounds used in the synthesis of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4-phenoxyphenyl)-1H-imidazo[4,5-c]pyridin-2(3H)-one.
专利号:EP-2167673-B1 优先权日:2007-06-25 标题:Process for the conversion of c-terminal peptide esters or acids to amides employing subtilisin in the presence of ammonium salts 发明人:EGGEN IVO FRANCI; BOERIU CARMEN G 权利人:ORGANON NV 摘要:The present invention relates to a process for the amidation of C-terminal esters or acids of peptide substrates in solution-phase synthesis of peptides, comprising amidating one or more peptide substrates comprising C-terminal esters or acids using the protease subtilisin in any suitable form in the presence of an ammonium salt derived from an acid having a pKa above 0. This process is useful in the production of protected or unprotected peptides.
专利号:US-11390645-B2 优先权日:2016-08-08 标题:Process for the preparation of 3β-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene 发明人:BARBIERI FRANCESCO; LENNA ROBERTO 权利人:IND CHIMICA SRL 摘要:A process for the synthesis of β-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (6).
[参考文献]: Carina S D Wink, Et Al. Lefetamine, A Controlled Drug And Pharmaceutical Lead Of New Designer Drugs: Synthesis, Metabolism, And Detectability In Urine And Human Liver Preparations Using Gc-Ms, Lc-Ms(N), And Lc-High Resolution-Ms/ms. Anal Bioanal Chem. 2015 Feb;407(6):1545-57. [参考文献]: Jun Hu, Et Al. An Olive-Shaped Sno2 Nanocrystal-Based Low Concentration H2S Gas Sensor With High Sensitivity And Selectivity. Phys Chem Chem Phys. 2015 Aug 28;17(32):20537-42. [参考文献]: Paul A Nakata, Et Al. An Assessment Of Engineered Calcium Oxalate Crystal Formation On Plant Growth And Development As A Step Toward Evaluating Its Use To Enhance Plant Defense. Plos One. 2015 Oct 30;10(10):E0141982. [参考文献]: Radomír Pilny, Et Al. Thermodynamics For Complex Formation Between Palladium(Ii) And Oxalate. Dalton Trans. 2014 Aug 28;43(32):12243-50.
合成参考文献
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 186. 参考文献:10.1007/s11356-020-10188-2 摘要:Mulder I, Schmittdiel M, Frei H, Hofmann L, Gerbig D, Siemens J. Soil water solutes reduce the critical micelle concentration of quaternary ammonium compounds. Environmental Science and Pollution Research. 2020 Aug 12;27(36):45311–23. doi: 10.1007/s11356-020-10188-2. 参考文献:10.1007/s00425-002-0759-8 摘要:McConn MM, Nakata PA. Calcium oxalate crystal morphology mutants from Medicago truncatula. Planta. 2002 Jul;215(3):380–6. doi: 10.1007/s00425-002-0759-8.