A novel method for synthesis of 2-butyl-5 -chloro-3H-imidazole-4-carbaldehyde 2, a key intermediate of Losartan was reported. The compound 2 was synthesized from starting material dimethyl malonate 6 and n-valeronitri...A novel method for synthesis of 2-butyl-5 -chloro-3H-imidazole-4-carbaldehyde 2, a key intermediate of Losartan was reported. The compound 2 was synthesized from starting material dimethyl malonate 6 and n-valeronitrile 8 by six steps with an overall yield of 40%. The key step including the reaction of compound 5 with POCl3/DMF followed by hydrolysis to give compound 2 with the yield of 68%.展开更多
A first total synthesis of isoliquiritin was accomplished starting from p-hydroxybenzaldehyde and 2,4-dihydroxyacetylphenone. The key step is condensation reaction. In synthetic process need not protect the hydroxy gr...A first total synthesis of isoliquiritin was accomplished starting from p-hydroxybenzaldehyde and 2,4-dihydroxyacetylphenone. The key step is condensation reaction. In synthetic process need not protect the hydroxy group of reacting substance.展开更多
β-Bromovinyl tellurides are new difuctional reagents which undergo palladium-catalyzed cross-coupling reaction with alkenes to give conjugated dienyl tellurides.
A series of 4H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides was designed, synthesized and evaluated against vesicular stomatitis virus （VSV） in Wish cell. The antiviral activities of all compound...A series of 4H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides was designed, synthesized and evaluated against vesicular stomatitis virus （VSV） in Wish cell. The antiviral activities of all compounds were stronger than those of acyclovir, while their toxicities were similar to those of acyclovir.展开更多
A novel and practical synthetic route is presented for the preparation of methyl-（E）-2-（3-（3-（2-（7-chloro-2-quinolinyl）ethenyl） phenyl）-3-oxopropyl）benzoate,the key intermediate of Montelukast,a leukotriene ...A novel and practical synthetic route is presented for the preparation of methyl-（E）-2-（3-（3-（2-（7-chloro-2-quinolinyl）ethenyl） phenyl）-3-oxopropyl）benzoate,the key intermediate of Montelukast,a leukotriene antagonist.The main diarylpropane framework was prepared via a polarity conversation reaction resulting in an acyl anion equivalent followed by a nucleophilic substitution reaction.The overall yield of this approach was 61%.This method is simple for operation and suitable for industrial production.展开更多
New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were ev...New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were evaluated.It was demonstrated that most of compounds had stronger antiviral acitivity than acyclovir,while their toxicities were similar or lower to acyclovir.展开更多
A novel and efficient synthetic method of atorvastatin was described.The key step of the synthesis was the construction of the olefin linkage between the chiral side chain and skeleton via a Horner-Wadsworth-Emmons re...A novel and efficient synthetic method of atorvastatin was described.The key step of the synthesis was the construction of the olefin linkage between the chiral side chain and skeleton via a Horner-Wadsworth-Emmons reaction,resulting in the advanced intermediate of atorvastatin under hydrogenation of the olefin over Pd/C.This novel method is more useful for the practical synthesis of atorvastatin than its document reported methods.展开更多
基金supported by Outstanding Youth Foundation of Heilongjiang Province(No.JC200706)
文摘A novel method for synthesis of 2-butyl-5 -chloro-3H-imidazole-4-carbaldehyde 2, a key intermediate of Losartan was reported. The compound 2 was synthesized from starting material dimethyl malonate 6 and n-valeronitrile 8 by six steps with an overall yield of 40%. The key step including the reaction of compound 5 with POCl3/DMF followed by hydrolysis to give compound 2 with the yield of 68%.
文摘A first total synthesis of isoliquiritin was accomplished starting from p-hydroxybenzaldehyde and 2,4-dihydroxyacetylphenone. The key step is condensation reaction. In synthetic process need not protect the hydroxy group of reacting substance.
基金This work was supported by Natural Science Foundation of Zhejiang Province.
文摘β-Bromovinyl tellurides are new difuctional reagents which undergo palladium-catalyzed cross-coupling reaction with alkenes to give conjugated dienyl tellurides.
基金the National Natural Science Foundation of China(No.30572240).
文摘A series of 4H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleosides was designed, synthesized and evaluated against vesicular stomatitis virus （VSV） in Wish cell. The antiviral activities of all compounds were stronger than those of acyclovir, while their toxicities were similar to those of acyclovir.
基金supported by the National Key Project for Basic Research(No2010CB1126102)the Outstanding Youth Foundation of Heilongjiang Province(NoJC200706)
文摘A novel and practical synthetic route is presented for the preparation of methyl-（E）-2-（3-（3-（2-（7-chloro-2-quinolinyl）ethenyl） phenyl）-3-oxopropyl）benzoate,the key intermediate of Montelukast,a leukotriene antagonist.The main diarylpropane framework was prepared via a polarity conversation reaction resulting in an acyl anion equivalent followed by a nucleophilic substitution reaction.The overall yield of this approach was 61%.This method is simple for operation and suitable for industrial production.
基金the National Natural Science Foundation of China(No.30572240)
文摘New pyrimidine nucleoside derivatives with nitric oxide（NO） donor were systematically synthesized.The antivirus activities of these nucleoside analogues against vesicular stomatitis virus（VSV） in Wish cell were evaluated.It was demonstrated that most of compounds had stronger antiviral acitivity than acyclovir,while their toxicities were similar or lower to acyclovir.
基金the financial supports from the National Key Project for Basic Research(No.2010CB 11261 02)the Outstanding Youth Foundation of Heilongjiang Province(No.JC200706)
文摘A novel and efficient synthetic method of atorvastatin was described.The key step of the synthesis was the construction of the olefin linkage between the chiral side chain and skeleton via a Horner-Wadsworth-Emmons reaction,resulting in the advanced intermediate of atorvastatin under hydrogenation of the olefin over Pd/C.This novel method is more useful for the practical synthesis of atorvastatin than its document reported methods.
