专利号:US-2025179012-A1 优先权日:2022-03-04 标 题:Synthesis of sulfur(vi) compounds and reagents for same 发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.
专利号:US-9284266-B2 优先权日:2012-01-19 标题:Method for synthesizing ramalin and ramalin precursor by using glutamic acid derivative and hydroxy aniline or hydroxy aniline having protected hydroxy group 发明人:YIM JOUNG HAN; KIM IL CHAN; KIM DOCKYU; HAN SE JONG; LEE HYOUNG SEOK; BHATTARAI HARI DATTA; KIM TAI KYOUNG; KIM KEUN SIK 权利人:YIM JOUNG HAN; KIM IL CHAN; KIM DOCKYU; HAN SE JONG; LEE HYOUNG SEOK; BHATTARAI HARI DATTA; KIM TAI KYOUNG; KIM KEUN SIK; KOREA INST OF OCEAN SCIENCE AND TECHNOLOGY 摘要:Disclosed is a method of the synthesis of ramalin. It comprises reacting a glutamic acid derivative, which is prepared using alkylchloroformate, with a hydrazine salt compound, which is prepared from hydroxy aniline, whether protected or not. The synthesis method allows ramalin, excellent in antioxidant and anti-inflammatory activity, to be simply synthesized at stable yield even without use of a highly toxic solvent such as DMF. In addition, the method is cost competitive, and provides ramalin at high efficiency, thus enabling the mass production of ramalin.
专利号:US-6916949-B2 优先权日:2001-01-29 标 题 :Methods of chemical systhesis of phenolic nitrogen mustard prodrugs 发明人:SPRINGER CAROLINE JOY; NICULESCU-DUVAZ DAN 权利人:CANCER REC TECH LTD 摘要:This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X2 is a halo group, and is -F, -Cl, -Br, or -I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic estenfication (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).
专利号:WO-02060862-A1 优先权日:2001-01-29 标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs
专利号:EP-1355876-B1 优先权日:2001-01-29 标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs
专利号:EP-1355876-A1 优先权日:2001-01-29 标题 :Methods of chemical synthesis of phenolic nitrogen mustard prodrugs
[参考文献]: Catherine Roullier, Et Al. A Novel Aryl-Hydrazide From The Marine Lichen Lichina Pygmaea: Isolation, Synthesis Of Derivatives, And Cytotoxicity Assays. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4582-6.
合成参考文献
摘要:Nahra, F.; Cazin, C. S. J., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 305.