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公开(公告)号：US5789599A
公开(公告)日：1998-08-04
申请号：US239097
申请日：1994-05-06
IPC分类号： C07C315/02 , C07C317/46 , C07C319/20 , C07C323/41 , C07D203/08 , C07D203/24
CPC分类号： C07D203/08 , C07C315/02 , C07C319/20 , C07D203/24
摘要： Novel N-sulfinyl-2-carboxyaziridine compounds and novel N-hydrogen-2-hydroxymethylaziridine compounds are provided. The asymmetric synthesis of N-sulfinylaziridines is readily accomplished in high diastereomeric purity and good yield by the Darzens-type reaction of the metal enolate of an .alpha.-haloester and an enantiopure sulfinimine. Ring-opening of these aziridines affords .alpha.-amino acids and the otherwise difficult to prepare syn-.beta.-hydroxy-.alpha.-amino acids, both key structural units found in many bioactive materials. The N-sulfinyl radical may be selectively removed from the novel aziridine compounds by treatment with acid or base. Alternatively, the N-sulfinyl radical may be oxidized to provide the corresponding N-sulfonyl-aziridine, or reduced to form the corresponding 1H-2-hydroxymethylaziridine, either of which may subsequently be ring-opened to provide precursors to bioactive compounds.
摘要翻译： 提供新的N-亚磺酰基-2-羧基氮丙啶化合物和新的N-氢-2-羟基甲基氮丙啶化合物。 N-亚氨基氮丙啶的不对称合成通过α-卤代醇金属烯醇化物和对映异构体亚硫酰亚胺的Darzens型反应，以高非对映纯度和良好的收率容易地实现。 这些氮丙啶的开环提供α-氨基酸，否则难以制备顺式-β-羟基-α-氨基酸，这是许多生物活性材料中发现的关键结构单元。 通过用酸或碱处理可以从新的氮丙啶化合物中选择性地除去N-亚硫酰基。 或者，N-亚硫酰基可被氧化以提供相应的N-磺酰基 - 氮丙啶，或还原形成相应的1H-2-羟甲基氮丙啶，其中之一可随后被开环以提供生物活性化合物的前体。
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公开(公告)号：US20120329828A1
公开(公告)日：2012-12-27
申请号：US13475292
申请日：2012-05-18
IPC分类号： C07D451/12 , A61P23/00 , A61P25/24 , A61K31/46
CPC分类号： C07D471/08
摘要： The invention provides novel cocaine analogs. The invention also provides a method of preparing cocaine analogs with control over the substituents installed at the C-1, C-2, C-3, C-4 and N-8 positions of the tropane bicyclic scaffold. The invention further provides methods of providing anesthesia, blocking reuptake of a monoamine neurotransmitter, and treating depression, by administering to a subject in need of such treatment a pharmaceutical composition comprising a compound of the invention.
摘要翻译： 本发明提供了新的可卡因类似物。 本发明还提供了一种制备可卡因类似物的方法，所述可卡因类似物具有对安置在托烷双环支架的C-1，C-2，C-3，C-4和N-8位置上的取代基的控制。 本发明还提供了通过向需要这种治疗的受试者施用包含本发明化合物的药物组合物来提供麻醉，阻断单胺神经递质再摄取和治疗抑郁症的方法。
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公开(公告)号：US5041670A
公开(公告)日：1991-08-20
申请号：US174663
申请日：1988-03-29
IPC分类号： C07C209/62
CPC分类号： C07C209/62
摘要： Methods of producing N-phenyl amines comprise reacting a phenyl-containing isocyanate with HR, and a boron complexing agent in an aprotic solvent, wherein R, is --OH or --COOH (i.e., water or formic acid), neutralizing the resulting N-aryl amide to N-aryl amine and recovering the N-aryl amine.
摘要翻译： 生产N-苯基胺的方法包括使含苯基的异氰酸酯与HR反应，和硼络合剂在非质子传递溶剂中反应，其中R 1为-OH或-COOH（即水或甲酸），中和得到的N- 芳基酰胺转化成N-芳基胺并回收N-芳基胺。
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公开(公告)号：US5260483A
公开(公告)日：1993-11-09
申请号：US756420
申请日：1991-09-09
IPC分类号： C07C231/10 , C07C233/05
CPC分类号： C07C231/10
摘要： Methods of producing N-aryl amides comprise reacting an aromatic isocyanate compound with substantially anhydrous carboxylic acid and recovering the resulting N-aryl amide. Additionally, or alternatively, methods of forming N-aryl amides comprise reacting an aromatic isocyanate compound with substantially anhydrous carboxylic acid in the presence of an anhydrous hydrogen halide or hydrolytically unstable halide compound and recovering the resulting N-aryl amide. These reactions may occur in the presence of an aprotic solvent.
摘要翻译： 制备N-芳基酰胺的方法包括使芳族异氰酸酯化合物与基本上无水的羧酸反应并回收所得的N-芳基酰胺。 另外或备选地，形成N-芳基酰胺的方法包括在无水卤化氢或水解不稳定的卤化物存在下使芳族异氰酸酯化合物与基本上无水的羧酸反应，并回收所得的N-芳基酰胺。 这些反应可能在非质子溶剂存在下进行。
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公开(公告)号：US08557842B2
公开(公告)日：2013-10-15
申请号：US13475292
申请日：2012-05-18
IPC分类号： C07D451/12 , A61K31/46 , A61P23/00 , A61P25/24
CPC分类号： C07D471/08
摘要： The invention provides novel cocaine analogs. The invention also provides a method of preparing cocaine analogs with control over the substituents installed at the C-1, C-2, C-3, C-4 and N-8 positions of the tropane bicyclic scaffold. The invention further provides methods of providing anesthesia, blocking reuptake of a monoamine neurotransmitter, and treating depression, by administering to a subject in need of such treatment a pharmaceutical composition comprising a compound of the invention.
摘要翻译： 本发明提供了新的可卡因类似物。 本发明还提供了一种制备可卡因类似物的方法，所述可卡因类似物具有对安置在托烷双环支架的C-1，C-2，C-3，C-4和N-8位置上的取代基的控制。 本发明还提供了通过向需要这种治疗的受试者施用包含本发明化合物的药物组合物来提供麻醉，阻断单胺神经递质再摄取和治疗抑郁症的方法。
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