在 Ammonium Hydroxide,N,N-二异丙基乙胺体系中,用 四氢呋喃 用作溶剂,化学反应 4.17H,反应生成4-氨基吡唑并[3,4-D]嘧啶 参考文献: Cyclic Di-Nucleotide Compounds And Methods Of Use[fr] Composés Di-Nucléotides Cycliques Et Leurs Procédés D'Utilisation 标题: Cyclic Di-Nucleotide Compounds And Methods Of Use[fr] Composés Di-Nucléotides Cycliques Et Leurs Procédés D'Utilisation 摘要:揭示了环二核苷酸cgamp类似物,合成这些化合物的方法,包括这些化合物的药物组合物,以及在医学治疗中使用这些化合物和组合物的用途.
专利信息
专利号:US-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-10882884-B2 优先权日:2016-05-18 标题:Stereoselective synthesis of phosphorothioate oligoribonucleotides 发明人:HALL JONATHAN; LI MEILING 权利人:ETH ZUERICH 摘要:The present invention relates to chiral phosphoramidites represented by formula (Ia) or formula (Ib) n n n n n n n n n n n n as novel monomers for the synthesis of stereodefined phosphorothioate MOE oligonucleotides. Furthermore, the present invention relates to a method for synthesizing stereodefined phosphorothioate MOE oligonucleotides using said novel chiral phosphoramidites.
专利号:US-11920040-B2 优先权日:2018-05-29 标 题 :Carborhodamine compounds and methods of preparation thereof 发明人:LUKHTANOV EUGENY A 权利人:ELITECHGROUP MDX LLC 摘要:The carborhodamine dyes disclosed herein are novel reagents suitable for automated incorporation of carborhodamine dyes into oligonucleotides that can be used in detection methods for nucleic acid targets. This disclosure provides an efficient and simple process for the preparation of carborhodamine compounds and introduces previously unknown reagents for the automated synthesis of oligonucleotide-carborhodamine conjugates.
专利号:US-7635772-B2 优先权日:2002-12-18 标 题 :Process for the preparation of oligonucleotides 发明人:MCCORMAC PAUL 权利人:AVECIA BIOTECHNOLOGY INC 摘要:A process for the synthesis of an oligonucleotide is provided in which an oligonucleotide is assembled on a swellable solid support using the phosphoramidite approach in the presence of an activator, wherein the activator is not tetrazole or a substituted tetrazole. Preferred activators are pyridinium, imidazolinium and benzimidazolinium salts; benzotriazole and derivatives thereof; and saccharin or a saccharin derivative. Preferred swellable solid supports comprise functionalised polystyrene, partially hydrolysed polyvinylacetate or poly(acrylamide).
专利号:WO-2020117135-A1 优先权日:2018-12-04 标 题:A process for preparation of 1h-pyrazolo[3,4-d] pyrimidine derivatives 发明人:HAAS PHILIPP DANIEL; STECKEL ANDREAS HARTWIG; BELLUR ATICI ESEN; ALTUNDAS RAMAZAN; OZTURK AYDIN BUSRA; SECEN HASAN; AYDIN BUSRA NUR 权利人:DEVA HOLDING AS 摘要:The present invention relates to an efficient and industrially advantageous process for the preparation of 1H-pyrazolo[3,4-d] pyrimidine derivatives. In particular the present invention provides a process for the preparation of 4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4- d]pyrimidine and tert-butyl (R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4- d]pyrimidin-1-yl)piperidine-1-carboxylate. Said compounds are important intermediates in the synthesis of ibrutinib. The method provided for preparing intermediates of ibrutinib has the advantages of a simple operation, high yield and low costs.
专利号:US-9790531-B2 优先权日:2012-08-14 标 题 :Enzymes and polymerases for the synthesis of RNA 发明人:WANG YUXUN; RAMAKRISHNAN DIVAKAR; DE FOUGEROLLES ANTONIN; WHORISKEY SUSAN 权利人:MODERNATX INC 摘要:The invention relates to compositions and methods for the design, evolution, preparation, and/or manufacture of enzymes for use with polynucleotides, primary transcripts and mmRNA molecules.
[参考文献]: Saha D, Et Al. Pyrazoloadenine Inhibitors Of The Ret Lung Cancer Oncoprotein Discovered By A Fragment Optimization Approach. Chemmedchem. 2021 May 18;16(10):1605-1608. [参考文献]: Skipper He, Et Al. Inhibition Of Experimental Neoplasms By 4-Aminopyrazolo (3, 4-D) Pyrimidine. Proc Soc Exp Biol Med. 1955 Aug;89(4):594-6. [参考文献]: Chih-Hang Anthony Tang, Et Al. Inhibition Of Er Stress-Associated Ire-1/xbp-1 Pathway Reduces Leukemic Cell Survival. J Clin Invest. 2014 Jun;124(6):2585-98. [参考文献]: Hideo Kubota, Et Al. Mglur1-Mediated Excitation Of Cerebellar Gabaergic Interneurons Requires Both G Protein-Dependent And Src-Erk1/2-Dependent Signaling Pathways. Plos One. 2014 Sep 2;9(9):E106316. [参考文献]: J M Andersen, Et Al. Cholesterogenesis: Derepression In Extrahepatic Tissues With 4-Aminopyrazolo (3,4-D) Pyrimidine. Science. 1976 Sep 3;193(4256):903-5.
合成参考文献
摘要:National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program., JAN1986 摘要:Proceedings of the Society for Experimental Biology and Medicine., 93(398), 1956 [] 摘要:Progress in Medical Chemistry., 7(69), 1970 [] 参考文献:10.1007/978-0-387-77570-8_12 摘要:Carter NS, Yates P, Arendt CS, Boitz JM, Ullman B. Purine and pyrimidine metabolism in Leishmania. Adv Exp Med Biol. 2008;625():141–54. doi: 10.1007/978-0-387-77570-8_12. 参考文献:10.1016/0006-2952(95)02070-5 摘要:Naguib FN, Iltzsch MH, el Kouni MM, Panzica RP, el Kouni MH. Structure-activity relationships for the binding of ligands to xanthine or guanine phosphoribosyl-transferase from Toxoplasma gondii. Biochem Pharmacol. 1995 Nov 09;50(10):1685–93. doi: 10.1016/0006-2952(95)02070-5.