专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
专利号:US-3947517-A 优先权日:1969-06-12 标题:Stereoselective introduction of tetracyclines hydroxyl group at 12(a) position in synthesis of tetracyclines 发明人:MUXFELDT HANS H; MICHAEL JEFFREY 权利人:RESEARCH CORP 摘要:In the synthesis of tetracyclines, a critical step is the stereospecific or stereoselective introduction of a hydroxyl group at the C-12(a) position, a novel method for the introduction of this critical hydroxy group is disclosed. Additionally, synthetic procedures for obtaining tetracycline precursors are discussed.
专利号:EP-4423083-A2 优先权日:2021-11-29 标 题:Synthesis of pyrazolone derivative compounds and their effects on cox enzymes 发明人:ÖNAY UÇAR EVREN; DEM RAYAK EREF; BERK BARKIN; YURTTA LEYLA; B LTEK N KALEL SEVDE NUR; AH N ZAFER 权利人:UNIV ISTANBUL MEDIPOL; ISTANBUL UNIV REKTORLUGU; ANADOLU UNIV 摘要:The invention is related to the synthesis of 8 pyrazolone derivative compounds and their activities on COX enzymes.
专利号:US-8552175-B2 优先权日:2009-04-23 标题:Sulfur transfer reagents for oligonucleotide synthesis 发明人:GUZAEV ANDREI P 权利人:GUZAEV ANDREI P; A M CHEMICALS INC 摘要:The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones, 5-phenyl-3H-1,2,4-dithiazole-3-thiones, and derivatives thereof as novel, efficient sulfur-transfer reagents is disclosed. Sulfur transfer from these reagents to compounds containing a P(III) atom (e.g., triphenylphosphine, 5′-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5′-O-DMT-3′-O-levulinyl dithymidilyl 2-cyanoethyl phosphite), was studied in solution by 31 P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2′-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods. As opposed to many sulfur transfer reagents known in the prior art such as 1,2-benzodithiol-3-one-1,1-dioxide (Beaucage reagent) and 5-ethoxy-3H-1,2,4-dithiazole-2-one (EDIT), the sulfurizing agents disclosed herein are highly stable in solution, which increases their practical and commercial value.
专利号:US-2023303546-A1 优先权日:2020-03-05 标题:Process And Intermediates For The Preparation Of Pyroxasulfone 发明人:RECSEI CARL; BARDA YANIV 权利人:ADAMA AGAN LTD 摘要:The invention relates to a process for preparing a key intermediate of Formula (I) in the synthesis of pyroxasulfone. The process comprises reacting an isoxazole of Formula (II) with a thionating reagent to create an S-substituted thioisoxazole of Formula (III); and combining the S-substituted thioisoxazole of Formula (III) with a pyrazole of the Formula (IV) by introducing a methylene bridge, to obtain a compound of Formula (I). The invention also relates to novel S-substituted thioisoxazole of Formula (III) and processes of preparation thereof, wherein L1 is halogen or an anionic residue derived from an acid; R is an organic residue derived from a suitable thionating reagent: dimethyl thioformamide, thiosulfate salts, dithiooxamide, alkyl xanthate salts, thiobenzamide, V-substituted thiourea and thioacetate salts.
专利号:US-8927584-B2 优先权日:2011-02-22 标 题:Synthesis of 2-(4-aminophenyl)benzothiazole derivatives and use thereof 发明人:WANG JEH-JENG; LIAO CHAO-CHENG; Hu wan-ping; SHEN HO-CHUAN 权利人:UNIV KAOHSIUNG MEDICAL 摘要:The present invention provides a photodynamic therapy to a patient having at least one tumor comprising the steps of: administering a compound of formula 6 (wherein R 1 and R 2 are defined as the above) in a pharmaceutically acceptable carrier to the patient; waiting for a sufficient time to allow the administered compound to be taken up by a target tissue having the at least one tumor; and irradiating a region of the patient containing the target tissue, wherein growth of the tumor is inhibited.
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合成参考文献
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