Oxybutynin Chloride

Researchers have developed a unique catalyst that promises to revolutionize drug synthesis. It overcomes a common problem associated with the production of drugs from ketones. Using their catalyst, the researchers synthesized a key component of the commonly used incontinence drug oxybutynin. Their results underscore the potential of the catalyst to improve drug discovery and development. A research group at Nagoya University in Japan has developed a new catalyst that promises to revolutionize the asymmetric synthesis of pharmaceuticals called chiral macrocyclic dilithium(I) salt. It overcomes the lack of reactivity of ketones and the difficulty inducing them to arrange atoms, which are common challenges in drug-making. The researchers used their technique to synthesize a key intermediate of the incontinence drug oxybutynin. Their catalyst promises to contribute to future drug discovery and development. They published their results in the Journal of the American Chemical Society. "This research represents a major advance in chiral drug synthesis," said Professor Ishihara from Nagoya University. "Our catalyst can facilitate the rapid synthesis of complex compounds. This holds great promise for future drug discovery efforts." All drugs are made from precursor chemicals. Ideal precursors are versatile compounds that can create a wide variety of end products. One particularly versatile precursor is optically active tertiary propargyl alcohol. It is used to create pharmaceuticals, including anticancer agents, antibiotics, and antivirals. However, production of these important chemicals is hindered by the low reactivity of ketones, which are precursors of tertiary propargyl alcohols. In addition, there is the difficulty of their asymmetric induction, a process that favors the creation of a specific arrangement of atoms that is more suitable than other arrangements for making the drug. To overcome the low reactivity of the ketones, highly reactive lithium-based reactants, called lithium acetylides, are added. However, their reactivity is often insufficient for use with ketones. The development of a new catalyst was needed to promote the reaction and control the selection of the optimal arrangement of atoms. Enzymes are ideal for these reactions, as they lower the energy required to make the reaction occur. However, due to their large and complicated structure, the synthesis of enzymes is difficult. The currently used acyclic dilithium catalyst-based approach was pioneered by Kumamoto University's Makoto Nakajima. However, this approach has a limited substrate scope due to the self-aggregation of catalysts and an overly long reaction time of up to 12 hours. This creates a bottleneck when producing the desired drug. Professor Kazuaki Ishihara and his collaborators, which included his graduate students, developed a chiral macrocyclic dilithium(I) salt. It is a simple catalyst that functions like an enzyme, overcoming the decrease in reactivity by activating less reactive ketones. This allows the addition of acetylides, such as lithium acetylides. The large macrocyclic structure of the catalyst allows them to catalyze even bulky ketones. This prevents aggregation between the catalyst and the lithium-based reactants. Despite being simpler than enzymes, the researchers found that their catalyst was more efficient than other known catalysts. They successfully synthesized optically active tertiary propargyl alcohol from a variety of ketones. Although this industrial alcohol is difficult to produce by conventional methods, they synthesized it in 5 to 30 minutes. This is much faster than the 12 hours that Nakajima's catalyst-based production process takes. The addition of alkynyls to carbonyl compounds, such as ketones, is a valuable synthetic method for the preparation of versatile chiral alcohols that are widely found in pharmaceuticals and natural products. This research is a breakthrough in modern synthetic organic chemistry and a promising leap forward in drug discovery.

2024.1.12 • 海南海口【2024 MAH B证企业论坛】苏州高迈药业有限公司成立于2018年，即将搬迁至生物医药产业园四期，研发场地面积11000平方米；专注于外用药的药学研发（乳膏，软膏，凝胶，外用溶液，贴剂）；团队由日本的技术、生产人员领衔，国内知名高校教授为顾问团队；核心管理人员均具有多年的研发管理经验；目前已有1个外用药项目获批，2个创新药的临床1期批件，已申报3个产品。公司致力于“高端仿制”“改良型新药”“自主创新药”三步走战略，打造专业外用药“第一股”。项目清单— 项目名称 — 1利丙双卡因乳膏（已获批） 2阿达帕林凝胶（已注册申报） 3夫西地酸乳膏（已注册申报） 4过氧苯甲酰凝胶（已注册申报） 5阿达帕林过氧苯甲酰凝胶 6克立硼罗软膏 7莫匹罗星软膏 8双氯芬酸二乙胺乳胶剂 9硝酸咪康唑乳膏10盐酸阿莫罗芬乳膏11盐酸特比萘芬乳膏12联苯苄唑溶液13盐酸特比萘芬喷雾剂14利多卡因喷雾剂15盐酸阿莫罗芬搽剂16糠酸莫米松乳膏17艾氟康唑外用溶液18盐酸特比萘芬涂膜剂19盐酸利多卡因凝胶20丙酸氟替卡松乳膏21雌二醇凝胶22雌二醇贴片23非那雄胺喷雾剂24利多卡因喷雾剂25尿素乳膏26卡泊三醇软膏27卢立康唑乳膏28氟比洛芬凝胶贴膏29氟维司群乳膏30复方多粘菌素B软膏31黄体酮阴道缓释凝胶32氟轻松氢醌维A酸乳膏33利多卡因丁卡因乳膏34曲安奈德益康唑乳膏35双氯芬酸钠贴剂36双氯芬酸依泊胺贴37美沙拉秦栓38利多卡因凝胶贴膏39洛索洛芬钠凝胶贴膏40洛索洛芬钠贴剂41阿昔洛韦氢化可的松乳膏42利多卡因丙胺卡因气雾剂43多磺酸粘多糖乳膏44伊维菌素乳膏45盐酸丁卡因凝胶46克霉唑阴道乳膏47布洛芬乳膏48磷酸芦可替尼乳膏49克拉司酮乳膏50氢醌乳膏51曲咪新乳膏52双唑泰乳膏53奥昔布宁透皮贴剂54妥洛特罗贴剂55硝呋太尔制霉菌素阴道软膏56硝酸益康唑喷雾剂57盐酸氨酮戊酸外用散58复方倍氯米松樟脑乳膏59地奈德乳膏60酮洛芬凝胶设备及资质流变仪01透皮仪02粘度计03联系我们联系人 ：陈先生 18006207168↓↓快速报名通道↓↓▼             本次会议议程，可上下滑动查看9:00-9:20海南省医药产业政策介绍海南省工业和信息化厅专家09:20-09:50新政实施后，如何办B证？药监专家09:50-10:10茶歇10:10-10:40最新B证监管政策解读药监专家10:40-11:10MAH制度下企业仿制药立项王立峰  慧药咨询创始人11:10-11:40批文&项目合作路演11:40-13:30午餐时刻13:30-14:00医改政策盘点及企业应对策略许金灿，药闻康策创始人兼总经理14:00-14:30MAH委托生产-监管政策的解读沈红梅，重庆博腾制药科技股份有限公司制剂研发副总经理、正高级工程师14:30-15:00MAH B证企业经验谈销售型企业转型B证经验谈综合型药企持证委托生产经验谈研发型药企持证经验谈15:00-15:30批文&项目合作路演15:30-15:50茶歇15:50-16:20MAH B证公司迎接检查注意点周鹏程，国家资深GMP检查员16:20-16:50MAH制度下，B证企业委托生产共线风险考量唐老师，国家资深GMP检查员