以三甲胺、1,4-重氮二环[2,2,2]辛烷(DABCO)为催化剂,室温合成了19个Baylis-Hillman加成物(BH),生物活性测试发现:在2000 g a.i./ha的剂量下,2-((2,4-二氯苯基)(羟基)甲基)丙烯酸甲酯(BH-7)具有较为广谱的除草活性,对阔叶杂草百日草和...以三甲胺、1,4-重氮二环[2,2,2]辛烷(DABCO)为催化剂,室温合成了19个Baylis-Hillman加成物(BH),生物活性测试发现:在2000 g a.i./ha的剂量下,2-((2,4-二氯苯基)(羟基)甲基)丙烯酸甲酯(BH-7)具有较为广谱的除草活性,对阔叶杂草百日草和苘麻的防效达到100%;对禾本科杂草稗草和马唐的防效分别为80%和75%;在25g a.i./ha的剂量下3-(羟基(4-硝基苯基)甲基)丁-3-烯-2-酮(BH-18)对番茄晚疫病的防效为100%,对稻瘟病及蔬菜灰霉病的防效均为50%。展开更多
A facile and convenient protocol was developed for the synthesis of 1,5-diarylpyrazoles using Baylis-Hillman adducts in the presence of HY-zeolite as an efficient recyclable heterogeneous catalyst in reasonable reacti...A facile and convenient protocol was developed for the synthesis of 1,5-diarylpyrazoles using Baylis-Hillman adducts in the presence of HY-zeolite as an efficient recyclable heterogeneous catalyst in reasonable reaction times(1.5-2.5 h) and high yields (78-90%).展开更多
A convenient method has been developed toward the stereoselective synthesis of N-substituted benzotriazole derivatives under mild conditions. The good stereolectivity, high yields and the simple procedure make the pre...A convenient method has been developed toward the stereoselective synthesis of N-substituted benzotriazole derivatives under mild conditions. The good stereolectivity, high yields and the simple procedure make the present protocol attractive.展开更多
A simple and convenient procedure for stercoselective synthesis of (Z)-allyl selenides has been developed by a one-pot reaction of diselenides with Baylis-Hillman adducts in the presence of samarium metal-trimethyls...A simple and convenient procedure for stercoselective synthesis of (Z)-allyl selenides has been developed by a one-pot reaction of diselenides with Baylis-Hillman adducts in the presence of samarium metal-trimethylsilyl chloride under mild conditions. Presumably, the diselenides are cleaved by Sm/TMSCI system to form selemde anions, which then undergo SN2' substitution of Baylis-Hillman adducts to produce the (Z)-allyl selenides.展开更多
A new thermomorphic catalytic system for the Baylis-Hillman coupling of aromatic aldehydes with a, β-unsaturated ketone has been described, in which the alkyl-functionalized dendritic catalyst preferred to dissolve i...A new thermomorphic catalytic system for the Baylis-Hillman coupling of aromatic aldehydes with a, β-unsaturated ketone has been described, in which the alkyl-functionalized dendritic catalyst preferred to dissolve in non-polar organic layer in the thermomorphic biphasic system, leading to easy separation of the catalyst from the polar products by changing the temperature of the system at end of the reaction.展开更多
Stereoselective transformation of Baylis-Hillman acetates I into corresponding (Z)-allyl iodides 2 has been achieved by treatment of I with samarium triiodide in THF. Remarkable rate acceleration of samarium triiodi...Stereoselective transformation of Baylis-Hillman acetates I into corresponding (Z)-allyl iodides 2 has been achieved by treatment of I with samarium triiodide in THF. Remarkable rate acceleration of samarium triiodide-mediated iodination of 1 was found when ionic liquid 1-n-butyl-3-methyl-imidazolium tetrafluroborate ([bmim]BF4) was used as reaction media in stead of THF. This novel approach proceeds readily at 50 ℃ within a few minutes to afford (Z)-allyl iodides 2 in excellent yields. A mechanism involving stereoselective iodination of the acetates of Baylis-Hillman adducts by samarium triiodide is described, in which a six-membered ring transition state played a key role in the stereoselective formation of 2.展开更多
Chiral activated alkene, L-menthyl acrylate and (+)-N-α-phenylethyl acrylamide, induced asymmetric Baylis-HiUman reaction of aromatic aldehydes was realized at 25℃ for 7 days in Me3N/H2O/solvent homogeneous mediu...Chiral activated alkene, L-menthyl acrylate and (+)-N-α-phenylethyl acrylamide, induced asymmetric Baylis-HiUman reaction of aromatic aldehydes was realized at 25℃ for 7 days in Me3N/H2O/solvent homogeneous medium. The corresponding Baylis-Hillman adducts were obtained in good chemical yield with moderate to excellent diastereoselectivity (up to 99% de).展开更多
文摘以三甲胺、1,4-重氮二环[2,2,2]辛烷(DABCO)为催化剂,室温合成了19个Baylis-Hillman加成物(BH),生物活性测试发现:在2000 g a.i./ha的剂量下,2-((2,4-二氯苯基)(羟基)甲基)丙烯酸甲酯(BH-7)具有较为广谱的除草活性,对阔叶杂草百日草和苘麻的防效达到100%;对禾本科杂草稗草和马唐的防效分别为80%和75%;在25g a.i./ha的剂量下3-(羟基(4-硝基苯基)甲基)丁-3-烯-2-酮(BH-18)对番茄晚疫病的防效为100%,对稻瘟病及蔬菜灰霉病的防效均为50%。
基金support from the Research Council of University of Guilan
文摘A facile and convenient protocol was developed for the synthesis of 1,5-diarylpyrazoles using Baylis-Hillman adducts in the presence of HY-zeolite as an efficient recyclable heterogeneous catalyst in reasonable reaction times(1.5-2.5 h) and high yields (78-90%).
基金the National Natural Science Foundation of China (No. 20072033)Specialized Research Fund for the Doctoral Program of Higher Education of China.
文摘A convenient method has been developed toward the stereoselective synthesis of N-substituted benzotriazole derivatives under mild conditions. The good stereolectivity, high yields and the simple procedure make the present protocol attractive.
基金Project (No. 2004C21032) supported by the Key Technologies R &D Program of Zhejiang Province, China
文摘A simple and convenient procedure for stercoselective synthesis of (Z)-allyl selenides has been developed by a one-pot reaction of diselenides with Baylis-Hillman adducts in the presence of samarium metal-trimethylsilyl chloride under mild conditions. Presumably, the diselenides are cleaved by Sm/TMSCI system to form selemde anions, which then undergo SN2' substitution of Baylis-Hillman adducts to produce the (Z)-allyl selenides.
文摘A new thermomorphic catalytic system for the Baylis-Hillman coupling of aromatic aldehydes with a, β-unsaturated ketone has been described, in which the alkyl-functionalized dendritic catalyst preferred to dissolve in non-polar organic layer in the thermomorphic biphasic system, leading to easy separation of the catalyst from the polar products by changing the temperature of the system at end of the reaction.
基金Project (No. 2004C21032) supported by the Key Technology R & DProgram of Zhejiang Province, China
文摘Stereoselective transformation of Baylis-Hillman acetates I into corresponding (Z)-allyl iodides 2 has been achieved by treatment of I with samarium triiodide in THF. Remarkable rate acceleration of samarium triiodide-mediated iodination of 1 was found when ionic liquid 1-n-butyl-3-methyl-imidazolium tetrafluroborate ([bmim]BF4) was used as reaction media in stead of THF. This novel approach proceeds readily at 50 ℃ within a few minutes to afford (Z)-allyl iodides 2 in excellent yields. A mechanism involving stereoselective iodination of the acetates of Baylis-Hillman adducts by samarium triiodide is described, in which a six-membered ring transition state played a key role in the stereoselective formation of 2.
基金the National Natural Science Foundation of China(20472033)the Ph.D.Programs of Ministry of Education of China(No.20020055002)for generous financial support for our programs.
文摘Chiral activated alkene, L-menthyl acrylate and (+)-N-α-phenylethyl acrylamide, induced asymmetric Baylis-HiUman reaction of aromatic aldehydes was realized at 25℃ for 7 days in Me3N/H2O/solvent homogeneous medium. The corresponding Baylis-Hillman adducts were obtained in good chemical yield with moderate to excellent diastereoselectivity (up to 99% de).