- An efficient synthesis of both enantiomers of Cathinone by regioselective reductive ring opening of substituted aziridines
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Both enantiomers of Cathinone were prepared as HCl salts from N-(R)-α-methylbenzylaziridine-2(S)-carboxaldehyde 2c and its enantiomer N-(S)-α-methyl-benzylaziridine-2(R)-carboxaldehyde 3c in high yield. This process makes it possible to prepare other aromatic and heteroaromatic analogs of Cathinone efficiently.
- Hwang, Gweon Il,Chung, Jae-Ho,Lee, Won Koo
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- Conjugate of cytotoxin molecule and cell binding receptor molecule
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A conjugate of a strong cytotoxin molecule and a cell binding receptor molecule has a structure shown in a molecular formula (I), wherein T, L, m, n, -----, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are defined in the text. The conjugate is used for treating cancer, immunological diseases and infectious diseases.
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- Conjugates of Cell Binding Molecules with Cytotoxic Agents
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A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9
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- CONJUGATE OF CELL-BINDING RECEPTOR WITH CYTOTOXIC AGENT
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PROBLEM TO BE SOLVED: To provide a conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule for targeted treatment. SOLUTION: According to the present invention, there is provided a conjugate having a structure of formula (I) and a pharmaceutical acceptable salt and a solvate thereof. The conjugate is used for treating cancer, autoimmune disease, and infectious disease. (T is a targeting or binding ligand; L is a releasable linker; a broken line is a linkage bond that L connects to a molecule inside the bracket independently; n is an integer of 1 to 20; m is an integer of 1 to 10; and a structure in parentheses is a potent antimitotic agent/drug.) SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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- CONJUGATES OF CELL BINDING MOLECULES WITH CYTOTOXIC AGENTS
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A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a formula (I), wherein T, L, m, n, Y, R1, R2, R3, R4, R5, R6, R7, R8, Rsu
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- Development and comparison of the substrate scope of Pd-catalysts for the aerobic oxidation of alcohols
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(Chemical Equation Presented) Three catalysts for aerobic oxidation of alcohols are discussed and the effectiveness of each is evaluated for allylic, benzylic, aliphatic, and functionalized alcohols. Additionally, chiral nonracemic substrates as well as chemoselective and diastereoselective oxidations are investigated. In this study, the most convenient system for the Pd-catalyzed aerobic oxidation of alcohols is Pd(OAc)2 in combination with triethylamine. This system functions effectively for the majority of alcohols tested and uses mild conditions (3 to 5 mol % of catalyst, room temperature). Pd(IiPr)(OAc)2(H2O) (1) also successfully oxidizes the majority of alcohols evaluated. This system has the advantage of significantly lowering catalyst loadings but requires higher temperatures (0.1 to 1 mol % of catalyst, 60°C). A new catalyst is also disclosed, Pd(IiPr)(OPiv)2 (2). This catalyst operates under very mild conditions (1 mol %, room temperature, and air as the O2 source) but with a more limited substrate scope.
- Schultz, Mitchell J.,Hamilton, Steven S.,Jensen, David R.,Sigman, Matthew S.
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p. 3343 - 3352
(2007/10/03)
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