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从天然植物制取(一)棉酚 总被引:1,自引:0,他引:1
本文首次报道从天然植物——海岛棉籽中分离出(-)棉酚。同时发现了受试的各种棉籽所含棉酚的光学活性的规律。(1)棉籽中棉酚的两个对映体(-)棉酚和(+)棉酚一般是不等量的,故其成分应为(±)棉酚和过量的(-)棉酚或(+)棉酚;(2)同种属棉籽含有相同旋光性的过量对映体,如海岛棉籽均含有过量的(-)棉酚,多数品种所含棉酚的光学纯度为10~25%,陆地棉籽则均含有过量的(+)棉酚,其相应棉酚的光学纯度为10~20%。 相似文献
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3-甲基芬太尼立体异构体的合成、绝对构型和镇痛活性 总被引:1,自引:0,他引:1
报道3-甲基芬太尼(2)四个光学异构体的合成及其绝对构型的确定,并测定了各异构体的镇痛活性(小鼠,ip,热板法)。结果表明,cis-(+)-(3R,4S)-2的镇痛作用最强,ED_(50)0.00767 mg/kg,镇痛效能是吗啡的2600倍,比其对映体cis-(-)-(3S,4R)-2以及混旋的cis-(±)-2分别强119和1.5倍;trans-(+)-(3S,4S)-2的镇痛效能是吗啡的450倍、trans-(-)-(3R,4R)-2的4倍。 相似文献
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Racemic, (-) and (+) gossypol, provided by the Department of Organic Chemistry of our institute, was suspended in 2.5% tween 80 solution. Adult male Wistar rats 190~220 g in weight were allotted to 5 groups. Animals in group 1 received 2.5% tween 80 solution as control. Rats in group 2 were treated with racemic gossypol at the dosage of 30 mg/kg for 2 weeks. Animals in group 3 and 4 were given 15 mg/kg of (-) gossypol for 2 weeks and 30 mg/kg of (-) gossypol for 1 week respectively. Rats in group 5 were treated with (+) gossypol at the dosage of 30 mg/kg for 2 weeks.Four weeks from the beginning of gossypol treatment the rats were cohabited with adult females for 7 days. Then the motility of the sperms in the cauda epididymides was estimated The female rats were examined for pregnancy 7 days later.Treatment with (-) gossypol at 30 mg/kg caused significant decreases in body weight of the rats (P<0.05). One of the five rats died 7 days after the last administration, while (+) gossypol and racemic gossypol at the dosage employed had no effect on the body weight. (+) Gossypol at 30 mg/kg for 2 weeks had no effect on the motility of the sperms in the cauda epididymides and no effect on the fertility of the animals: nor was there any effect on the weights of the testis, epididymis, prostate and seminal vesicle. The sperms of the cauda epididymides were found to be dead in the groups treated with 15 and 30 mg/kg of (-)gossypol. Raccmic gossypol given for 2 weeks at 30 mg/kg caused loss of fertility of the male rats which confirmed our previous findings.(?)t may be postulated that (+) gossypol has no antifertility effect nor toxicity at the dosage employed. (-) Gossypol is the active stereoisomer of racemic gossypol. 相似文献
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The reaction of racemic styrene oxide with deoxycytidine under aqueous conditions was studied. The four principal products isolated were a pair of diastereomeric N(4)-(2-hydroxy-1-phenylethyl)deoxycytidines ( approximately 20% of the products) and a pair of diastereomeric 3-(2-hydroxy-2-phenylethyl)deoxyuridines ( approximately 80% of the products). Reactions with optically active styrene oxides allowed the configurations of the 3-(2-hydroxy-2-phenylethyl)deoxyuridines to be assigned, and these structures were confirmed by an independent synthesis from deoxyuridine. Also, it was possible to tentatively assign the configurations of the N(4)-(2-hydroxy-1-phenylethyl)deoxycytidines that had undergone some racemization during the reaction (the ratio of the retained to inverted configuration of the products was approximately 1:7). 相似文献
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Yasuike S 《Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan》2003,123(7):577-585
The chemistry of chiral ligands for transition metal-catalyzed asymmetric reactions is an interesting research field in synthetic chemistry and has recently been the focus of much attention. Although a number of chiral ligands containing phosphorus (P) and arsenic (As) have been widely studied and are well documented, asymmetric reactions with optically active organoantimony compounds have not been reported so far. We are interested in the synthesis and utilization of optically active organoantimony compounds for asymmetric synthesis. We present here the synthesis and resolution of Sb-chiral and C2-symmetric compounds containing antimony as well as their physical and chemical properties. Resolution of (+/-)-1-phenyl-2-trimetylsilylstibindole (1), Sb (R/S)-(aryl) [2-(S)-(1-dimethylaminoethyl) phenyl] (p-tolyl) stibane (9), and (+/-)-2,2'-bis(diarylstibano)-1,1'-binaphthyl (13) can be achieved by the separation of a mixture of the diastereomeric antimony-palladium complexes. The optically pure Sb-chiral stibanes (1, 9) isolated here were optically stable, and no racemization on the chiral antimony center was observed even when they were heated under a neutral or a basic condition. Single-crystal X-ray analysis of Sb-chiral triarylstibane 9b-B revealed the presence of an intramolecular interaction between the antimony and nitrogen atoms. The optically active BINASb (13) can be used as powerful chiral ligand for the palladium-catalyzed asymmetric allylic alkylation of racemic 1,3-diphenyl-2-propen-1-yl acetate with dimethyl malonate. We also report the synthesis, molecular structure, and fluxional behavior of the (R)-(-)-7-p-tolyl-dinaphtho [2, 1-b; 1',2'-d] stibole (21c) which is the first isolated example of optically active C2-symmetric group 15 dinaphthoheteroles. 相似文献
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Asymmetric Reductive Amination of Cycloalkanones, XI1,2): Synthesis of Optically Active 2-Substituted Cycloheptanamines Asymmetric synthesis of 2-substituted cycloheptanamines from racemic cycloheptanones by means of reductive amination in a three-step procedure is described. Condensation of the ketones 1 with the optically active auxiliary R-(+)- or S-(-)-1-phenylethylamine leads to the imine mixtures 2 which are hydrogenated over Raney nickel to give the optically active, diastereomerically pure secondary amines 3 . Hydrogenolysis with Pd/C yields the optically active cis-2-substituted cycloheptanamines 4 . 相似文献
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Acylanilides, I: Syntheses of the Racemates and Enantiomers of Chiral Acylanilides The racemic and optically active cyanoacetyl chlorides 1 – 4 (R = Cl) or – in the presence of DCC – cyanoacetic acids 1 – 4 (R = OH) were reacted with p-phenetidine or 4-hydroxyaniline to give a series of racem. and optically active cyanoacyl anilides. With alkaline hydrogen peroxide 1a and 3a are converted to the malonic monoamide anilides 1c and 3c . The cyanoacyl anilide 2a was hydrogenated with high yield to 2-(aminomethyl)-2-isopropyl-4′-ethoxyvalerianyl anilide (2d) . The acyl anilides are to be tested pharmacologically. 相似文献
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The direct oxidation of a dipeptide azlactone (1) by DDQ affords an optically active unsaturated dipeptide azlactone (2). It was shown that the double bond had the Z-configuration and that no racemization of the proline moiety occurred during the oxidation. The dehydrotripeptide, Z-Pro-ΔPhe-Phe ˙ OH (9b) was prepared by direct coupling of azlactone (2) with phenylalanine tetramethyl-guanidinium salt and was shown to be stable to chymotrypsin. The tetrapeptide, Z-Pro-ΔPhe-His-Leu ˙ OH (11), was prepared directly from the azlactone (2) and by saponification of the tetrapeptide ester (10) prepared by mixed anhydride coupling of Z-Pro-ΔPhe ˙ OH (7) with the dipeptide ester. The dehydropeptide (11) inhibits angiotensin I converting enzyme (IC50, 1 × 10-4 M). 相似文献