Tert-Butyl (2-Amino-4,5-Dimethylphenyl)Carbamate置于palladium Dihydroxide 盐酸,氢气体系中,用 甲醇,水 作为反应溶剂,化学反应 7.0H,反应生成 5,6-二甲基苯并咪唑 参考文献:Formation Of The Dimethylbenzimidazole Ligand Of Coenzyme B12 Under Physiological Conditions By A Facile Oxidative Cascade 标题:Formation Of The Dimethylbenzimidazole Ligand Of Coenzyme B12 Under Physiological Conditions By A Facile Oxidative Cascade 摘要:Dimethylbezimidazole,The Axial Ligand Of Vitamin B-12,Is Synthesized From Riboflavin By A Two-Electron Oxidation,A Retro-Aldol Condensation,And A Second Two-Electron Oxidation. This Oxidative Cascade Readily Takes Place Nonenzymatically Under Physiological Conditions. DOI:10.1021/ol034530M
专利号:WO-0100609-A1 优先权日:1999-06-29 标题:Method for synthesis of n-homocysteine thiolactonyl retinamide 发明人:KAZIMIR MICHAEL; WILSON RAY E II 权利人:UNIV BAYLOR; KAZIMIR MICHAEL; WILSON RAY E II 摘要:The present invention describes methods of synthesis for N-homocysteine thiolactonyl retinamide (thioretinamide), a compound that has anticancer and antiatherogenic properties. The present invention further describes methods for the synthesis of N-homocysteine thiolactonyl retinamido cobalamin (thioretinaco), a compound that has potential anticancer, antineoplastic, antiviral, and antiatherogenic properties.
专利号:US-7951961-B2 优先权日:2006-07-07 标题:Enantioselective synthesis of pyrrolidines substituted with flavones, and intermediates thereof 发明人:SIVAKUMAR MEENAKSHI; SHUKLA MANOJ; JADHAV PRAMOD KUMAR; BORHADE AJIT 权利人:PIRAMAL LIFE SCIENCES LTD 摘要:The present invention relates to an enantioselective synthesis of (+)-trans enantiomer of pyrrolidines substituted with flavones, represented by Formula 1 or salts thereof, which are inhibitors of cyclin dependant kinases and can be used for treatment of proliferative disorders such as cancer n nwherein Ar has the meaning as indicated in the claims.
专利号:US-6531454-B1 优先权日:1999-03-16 标 题:Glycosylated polyamines and methods of use therefor 发明人:LEARY JULIE A; GAUCHER SARA P; PEDERSEN STEVEN F 权利人:UNIV CALIFORNIA 摘要:Glycosylated polyamines comprising of mono- or oligo-saccharides that are glycosidically linked to an aliphatic polyamine, and pharmaceutically acceptable salts, prodrugs and derivatives thereof are provided. An exemplary glycosylated polyamine has the following structure: n Glycosylated polyamines, their pharmaceutically acceptable salts, prodrugs and derivatives are useful, for example, as anticancer compounds for the treatment of a variety of cancers. Methods for synthesis of glycosylated polyamines are disclosed. In addition, metal complexes of glycosylated polyamines, the preparation of such metal complexes, analytical methods using the metal complexes are provided. Methods for detecting equatorial and axial conformation of a group other than hydrogen at the C2 position of a saccharide molecule are also provided. The compounds of the invention can be used as anti-cancer agents (e.g., against breast, ovarian, colon or renal cancers). Furthermore, the compounds of the invention are ligands for the estrogen receptor and thus can be used to modulate estrogen receptor activity, for example to treat or prevent breast cancer, to treat or prevent osteoporosis or to reduce the risk of cardiovascular disease in a subject (e.g., a postmenopausal female subject).
专利号:US-9884067-B2 优先权日:2013-03-14 标 题:Androgen receptor down-regulating agents and uses thereof 发明人:NJAR VINCENT C O; GEDIYA LALJI K; PURUSHOTTAMACHAR PURANIK; GODBOLE ABHIJIT; KWEGYIR AFFUL ANDREW; VASAITIS TADAS 权利人:UNIV OF MARYLAND EASTERN SHORE; UNIV JEFFERSON; UNIV MARYLAND 摘要:The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.
专利号:US-7777046-B2 优先权日:2007-03-20 标题:Method of synthesis of a salt of N-acetyl-L-cysteinylcobalamin 发明人:BRASCH NICOLA E; SUAREZ-MOREIRA EDWARD 权利人:UNIV KENT STATE OHIO 摘要:The invention provides a method for preparing the sodium salt of the novel thiol derivative of vitamin B 12 , N-acetyl-L-cysteinylcobalamin (Na[NACCbl]). The method involves carrying out the reaction in aqueous solvent with a relatively small excess of ligand reactant, specifically from one to less than four molar equivalents. The cobalamin derivative formed is precipitated from the aqueous solvent, preferably by the addition of a precipitate inducing solvent. This provides a product in acceptable purity without the need for an additional chromatographic purification step.
专利号:US-3935314-A 优先权日:1971-11-24 标题 :Anti-hypertensive compositions of benzimidazole derivatives 发明人:WATTS ERIC ALFRED 权利人:BEECHAM GROUP LTD 摘要:Antihypertensive pharmaceutical compositions comprising a compound of the formula (II) ##SPC1## n or pharmaceutically acceptable salts or solvates thereof wherein R 1 is nitrile or amidino; R 2 is hydrogen or lower hydrocarbon; R 3 , R 4 , R 5 and R 6 which may be the same or different, are each selected from hydrogen, halogen, nitro, trifluoromethyl, lower alkyl, lower acyl, hydroxyl, lower etherified hydroxyl or lower acylated hydroxyl; together with a pharmaceutically acceptable carrier. The compounds of formula (II) are also useful as intermediates in the synthesis of the corresponding 2-aminoimidazoline compounds.