专利号:US-5486615-A 优先权日:1993-11-30 标题:Method of making asymmetric DE ring intermediates for the synthesis of camptothecin analogs 发明人:COMINS DANIEL L 权利人:UNIV NORTH CAROLINA STATE 摘要:Methods of making asymmetric DE ring intermediates for the synthesis of camptothecin and camptothecin analogs employ a dioxane intermediate as the immediate precursor to the DE ring intermediate. Novel intermediates are also disclosed.
专利号:US-5488131-A 优先权日:1994-03-23 标题:Synthesis of compounds with predetermined chirality 发明人:MYERS ANDREW G 权利人:CALIFORNIA INST OF TECHN 摘要:A method for synthesizing enantiomerically enriched chemical intermediates with predetermined chirality is described. The method comprises formation of a pseudoephedrine amide, followed by stereoselective alkylation at the alpha carbon. The chiral auxiliary can then be cleaved off, affording chiral end products useful for further transformations. The enantiomeric enrichment of the chiral end products may exceed 98%, and the chiral auxiliary can be recovered. Novel amides of pseudoephedrine used in this method are also disclosed.
专利号:US-4727183-A 优先权日:1983-12-23 标题:Process for the asymmetric synthesis of chiral α-hydroxy-2-nitrobenzenepropanoic acid 发明人:BUZBY JR GEORGE C; WINKLEY MICHAEL W; MCCAULLY RONALD J 权利人:AMERICAN HOME PROD 摘要:Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C 1-4 alkyl or C 1-4 alkoxy, which comprises: n (a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid IV; n (b) reacting, respectively, said (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20° C., in order to obtain, respectively, and (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid IV; n (c) reducing the nitro group of said (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and n (d) cyclizing the resulting (R) or (S)-α-chloro-2-aminobenzenepropanoic acid in aqueous base.
专利号:US-5087691-A 优先权日:1989-09-01 标题 :Poly-phenylated diamines and their use as polycondensation monomers in the synthesis of polyamide, poly(amide-imide), and polyimide polymers 发明人:HARRIS FRANK W 权利人:UNIV AKRON 摘要:New polyphenylated polynuclear aromatic diamines, such as 1,3-bis[4-aminophenyl]-2,3,5-triphenylbenzene, a process for their manufacture and their use as polycondensation components for the manufacture of polyamide, polyamide-imide and polyimide polymers are described. The polymers obtained with the aromatic diamines according to the invention are readily soluble, rigid-rod polymers and are distinguished by outstanding modulus, tensile compression strength, energy absorption, coefficient of expansion and electrical properties.
专利号:US-4644081-A 优先权日:1985-02-11 标题:Process for the asymmetric synthesis of chiral indoline-2-carboxylic acids 发明人:BUZBY JR GEORGE C; WINKLEY MICHAEL W; MCCAULLY RONALD J 权利人:AMERICAN HOME PROD 摘要:Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C 1-4 alkyl or C 1-4 alkoxy, which comprises: n (a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid IV; n (b) reacting, respectively, said (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20° C., in order to obtain, respectively, and (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid IV; n (c) reducing the nitro group of said (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and n (d) cyclizing the resulting (R) or (S)-α-chloro-2-aminobenzenepropanoic acid in aqueous base.
专利号:US-4614806-A 优先权日:1983-12-23 标 题 :Process for the asymmetric synthesis of chiral indoline-2-carboxylic acids 发明人:BUZBY JR GEORGE C; WINKLEY MICHAEL W; MCCAULLY RONALD J 权利人:AMERICAN HOME PROD 摘要:Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C 1-4 alkyl or C 1-4 alkoxy, which comprises: n (a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid IV; n (b) reacting, respectively, said (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20° C., in order to obtain, respectively, and (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid IV; n (c) reducing the nitro group of said (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and n (d) cyclizing the resulting (R) or (S)-α-chloro-2-aminobenzenepropanoic acid in aqueous base.
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