专利号:US-5191087-A 优先权日:1991-07-24 标 题 :Process for the synthesis of 1,4-disubstituted pyrazoles 发明人:ALCARAZ JEAN-MARIE; LECACHEUR MARYSE; ROBIN YVES 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The present invention relates to a process for the synthesis of 1,4-disubstituted pyrazoles. A monosubstituted hydrazine is reacted with the product of reaction of an acetal with an N-substituted halomethyliminium salt, preferably N,N-dimethylchloromethyliminium chloride. n The 1,4-disubstituted pyrazoles are, in particular, important intermediates in the synthesis of herbicides or drugs.
专利号:WO-2024137329-A1 优先权日:2022-12-20 标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
专利号:US-11530204-B2 优先权日:2019-09-30 标 题 :Biocatalytic synthesis of cryptophycin anticancer agents 发明人:SHERMAN DAVID H; SCHMIDT JENNIFER J 权利人:UNIV MICHIGAN REGENTS 摘要:The disclosure provides cryptophycin intermediates, cryptophycin analogs, and cryptophycin chimeric molecules useful in treating cancer, as well as methods of producing these compounds and methods of treating cancer.
专利号:US-9901901-B2 优先权日:2012-05-21 标 题 :Selective extraction of anions from solution 发明人:MEZEI GELLERT 权利人:WESTERN MICHIGAN UNIV RESEARCH FOUNDATION; THE BOARD OF TRUSTEES OF WESTERN MICHIGAN UNIV 摘要:A method of selectively extracting anions from an aqueous solution using an anion encapsulating aggregate formed upon the addition of a solvent, a copper contributor, a hydroxide contributor, a counterion contributor, and pyrazole to an aqueous solution containing the anions, or upon the addition of a solvent, a polymeric chain of [Cu II (μ-OH)(μ-pz)] ∞ and a counterion contributor to the aqueous solution. The aggregates include compounds of the formula cis Cu II x (OR 1 ) y (R 2 pz) z , where R 1 is H or an alkyl group, R 2 is H, or an alkyl group or a charged group, pz is pyrazolate and each of x, y, and z is an integer between about 1 and about 40. In addition, ligand-containing anion encapsulating aggregates can be formed by synthesis with a lig-and-bound pyrazole or by substituting the ligand-bound pyrazole for the pyrazole incorporated in the aggregate.
专利号:WO-2023287345-A1 优先权日:2021-07-16 标 题 :Aqueous solid phase peptide synthesis 发明人:PAWLAS JAN; LUDEMANN-HOMBOURGER OLIVIER 权利人:POLYPEPTIDE LABORATORIES HOLDING PPL AB 摘要:The present invention relates to a solid phase peptide synthesis (SPPS) where the coupling of amino acids is performed in an aqueous solution comprising at least one organic co-solvent miscible with water. The aqueous solution is capable of sufficiently solubilize the activated Fmoc-α-amine protected amino acid or activated Fmoc-α-amine protected peptide fragment, and where the resin is capable of swelling in the presence of the aqueous solution above about 4 mLg-1. The invention also encompasses a method for regeneration of spent aqueous solution from the SPPS.
专利号:US-10226449-B2 优先权日:2013-12-20 标 题:Heterocyclic modulators of lipid synthesis and combinations thereof 发明人:HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
1: Zakharov S, Pelclova D, Navratil T, Belacek J, Komarc M, Eddleston M, Hovda KE. Fomepizole versus ethanol in the treatment of acute methanol poisoning: Comparison of clinical effectiveness in a mass poisoning outbreak. Clin Toxicol (Phila). 2015;53(8):797-806. doi: 10.3109/15563650.2015.1059946. Epub 2015 Jun 24. doi: 10.5507/bp.2014.056. Epub 2014 Nov 6. doi: 10.1016/j.pedneo.2013.08.009. Epub 2013 Dec 11. Japanese. doi: 10.3109/15563650.2012.716518. Epub 2012 Aug 14. doi: 10.3109/15563650.2012.683197. Epub 2012 May 4. doi: 10.1111/bcpt.12276. Epub 2014 Jun 18. Review. e3-5. doi: 10.1016/j.ajem.2010.11.014. Epub 2011 Jan 3.
合成参考文献
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 166. 摘要:Experientia., 28(1198), 1972 [] 摘要:Ahmad, O. K.; Movassaghi, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 195. 摘要:Zeitler, K., Science of Synthesis, (2019) , 329. 摘要:J. Elguero, E. Gonzalez and R. Jacquier. Bull. Soc. Chim. France 1968, 5009.