- Method for synthesizing 3 -butyne -2 - alcohol with high yield
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The invention discloses a method for synthesizing 3 -butyne -2 - alcohol, wherein tripolyacetaldehyde is used as a raw material acetaldehyde source, and potassium hydroxide or potassium tert-butoxide or potassium tert-butoxide is used as a dispersant. After the reaction endpoint material is hydrolyzed to remove potassium hydroxide, the target product 3 - butyne -2 - alcohol is separated by aqueous phase extraction. The method has the advantages of low acetylene reaction pressure. Target product yield is high.
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Paragraph 0033-0049
(2021/11/27)
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- Phosphine-Catalyzed Intermolecular Annulations of Fluorinated ortho-Aminophenones with Alkynones – The Switchable [4+2] or [4+2]/[3+2] Cycloaddition
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A phosphine-catalyzed intermolecular annulation reaction of functionalized ortho-aminoacetophenones with alkynones has been disclosed in this paper. A variety of 2-alkynylquinolines and benzo-fused indolizine were selectively afforded in moderate to good yields at different reaction temperatures and with different phosphine catalysts via the in situ generated zwitterionic intermediate derived from alkynone and phosphine. (Figure presented.).
- Zhang, Yanshun,Sun, Yaoliang,Wei, Yin,Shi, Min
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supporting information
p. 2129 - 2135
(2019/03/13)
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- Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib
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Three novel series of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib were prepared and evaluated in vitro for their cytostatic effects against a human chronic myeloid leukemia (K562), acute myeloid leukemia (HL60), and human leukemia stem-like cell line (KG1a). The structure-activity relationship was analyzed by determining the inhibitory rate of each imatinib analog. Benzene and piperazine rings were necessary groups in these compounds for maintaining inhibitory activities against the K562 and HL60 cell lines. Introducing a trifluoromethyl group significantly enhanced the potency of the compounds against these two cell lines. Surprisingly, some compounds showed significant inhibitory activities against KG1a cells without inhibiting common leukemia cell lines (K562 and HL60). These findings suggest that these compounds are able to inhibit leukemia stem-like cells.
- Li, Yong-Tao,Wang, Jing-Han,Pan, Cheng-Wen,Meng, Fan-Fei,Chu, Xiao-Qian,Ding, Ya-Hui,Qu, Wen-Zheng,Li, Hui-Ying,Yang, Cheng,Zhang, Quan,Bai, Cui-Gai,Chen, Yue
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p. 1419 - 1427
(2016/02/19)
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- Gold(I)-catalyzed decarboxylation of propargyl carbonates: Reactivity reversal of the gold catalyst from π-Lewis acidity to σ-Lewis acidity
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A cationic gold(I)-catalyzed decarboxylative etherification of propargyl carbonates to selectively produce propargyl ethers is reported. In the reaction the gold(I) catalyst shows a distinct σ-Lewis acidity rather than the commonly observed π-Lewis acidity, and thus catalyzes the decarboxylation of a variety of propargyl carbonates to give the corresponding propargyl ethers with high selectivity. This reaction represents a rare example of the tunable reactivity of cationic gold(I) complexes between σ-Lewis acidity and π-Lewis acidity.
- Shen, Ruwei,Yang, Jianjun,Zhu, Shugao,Chen, Chao,Wu, Luling
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supporting information
p. 1259 - 1269
(2015/04/22)
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- Palladacycle-catalyzed reaction of bicyclic alkenes with terminal ynones: Regiospecific synthesis of polysubstituted furans
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A new synthetic strategy to access polysubstituted furans regiospecifically has been developed using simple bicyclic alkenes and terminal ynones as starting materials with palladacycles as unique active catalysts. A rational mechanism has also been proposed. This reaction features mild reaction conditions, easily available starting materials and palladacycle catalysts, a wide substrate scope, and high regiospecificity.
- Ge, Guang-Cun,Mo, Dong-Liang,Ding, Chang-Hua,Dai, Li-Xin,Hou, Xue-Long
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supporting information
p. 5756 - 5759
(2013/01/15)
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- Novel sequential 1,4-Brook rearrangement-Wittig reaction: New one-pot approach for silyl dienol ethers
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A novel one-pot synthetic method of silyl dienol ethers via 1,4-Brook rearrangement-Wittig reaction sequence has been developed. This tandem reaction proceeded via the intramolecular silyl migration step, which enabled stereoselective formation of phosphorane intermediates. The reaction is operationally simple and high yielding, thus providing a new useful formula for silyl dienol ether synthesis.
- Matsuya, Yuji,Koiwai, Azusa,Minato, Daishiro,Sugimoto, Kenji,Toyooka, Naoki
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supporting information
p. 5955 - 5957,3
(2020/07/31)
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- N-Vinylpyridinium tetrafluoroborate salts as reagents for the stereoselective and regioselective synthesis of symmetrical (2E,4E)-1,6-dioxo-2,4-dienes
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We had previously demonstrated the utility of N-vinylpyridinium tetrafluoroborate salts as novel electrophilic coupling partners in Pd(0)-catalyzed Suzuki cross-coupling reactions with aryl and vinyl boronic acids. We now report that these crystalline, air-stable, and non-hygroscopic salts are also useful reagents for the synthesis of symmetrical (2E,4E)-1,6-dioxo-2,4-dienes (diene diones), which in turn are valuable starting materials for the synthesis of various five-membered heterocycles. The optimization of reaction conditions and the scope and limitations of the reductive dimerization are discussed.
- Gao, Ge,Brown, Neil,Minatoya, Machiko,Buszek, Keith R.
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scheme or table
p. 6491 - 6494
(2009/04/06)
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- On the viability of 5-endo-dig cyclisations of O-propargylic hydroxylamine derivatives, leading to 2,5-dihydroisoxazoles (3-isoxazolines)
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O-Propargylic hydroxylamines undergo smooth 5-endo-dig cyclisations upon exposure to 3 equiv of molecular iodine to give respectable yields of the corresponding 4-iodo-2,5-dihydroisoxazoles, which should find a number of applications as intermediates for syntheses amongst this useful class of heterocycles.
- Foot, Oliver F.,Knight, David W.,Low, Ai Cheng Lilian,Li, YingFa
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p. 647 - 650
(2007/10/03)
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- The trimethylsilyl xylyl (TIX) ether: A useful protecting group for alcohols
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A new protecting group for alcohols, the p-trimethylsilyl xylyl (TIX) group has been developed. The TIX group is used to protect various alcohols under acidic as well as basic conditions. The protected ethers thus formed had noteworthy chemoselectivity upon deprotection in the presence of other benzyl ethers and commonly used protecting groups. The stability of the TIX group towards various reagents has also been examined.
- Reddy, Ch. Raji,Chittiboyina, Amar G.,Kache, Rajashaker,Jung, Jae-Chul,Watkins, E. Blake,Avery, Mitchell A.
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p. 1289 - 1295
(2007/10/03)
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- Enantioselective synthesis of both enantiomers of various propargylic alcohols by use of two oxidoreductases
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The oxidoreductases Lactobacillus brevis alcohol dehydrogenase (LBADH) and Candida parapsilosis carbonyl reductase (CPCR) are suitable catalysts for the reduction of ketones to afford enantiopure sec. alcohols. A broad variety of alkynones (1, 3, and 5) are accepted as substrates and the corresponding propargylic alcohols (2, 4, and 6) are obtained in good yield and excellent enantiomeric excess. By changing the steric demand of the substituents the ee values can be adjusted and even the configurations of the products can be altered.
- Schubert, Thomas,Hummel, Werner,Kula, Maria-Regina,Mueller, Michael
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p. 4181 - 4187
(2007/10/03)
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- New chiral hosts derived from dimeric tartaric acid: Efficient optical resolution of aliphatic alcohols by inclusion complexation
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The novel, chiral, host compounds 8 and 9 were derived from tartaric acid. Inclusion complexation with these host compounds permitted highly efficient resolution of some aliphatic alcohols (10-13). The symmetrical dimer host compound 8 is effective for optical resolution of alcohols 10, 12, and 13 by a combination of enantioselective inclusion complexation and distillation techniques. The unsymmetrical dimer host compound 9 is effective for optical resolution of cyanohydrin 11. The crystal structures of the inclusion complexes were analyzed by X-ray diffraction methods in order to elucidate the mechanism of the efficient chiral recognition in the inclusion crystals.
- Tanaka, Koichi,Honke, Shinji,Urbanczyk-Lipkowska, Zofia,Toda, Fumio
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p. 3171 - 3176
(2007/10/03)
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- METHOD FOR TREATING ANXIETY
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The present invention provides a method for treating anxiety in humans using azacyclic or azabicyclic compounds.
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- HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE
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The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
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- HYDRATION TRIMERIZATION OF ACETYLENE IN SUPERBASIC MEDIA III. VINYLATION OF ACETYLENIC ALCOHOLS AS INTERMEDIATE STAGE
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It was confirmed that the hydration-trimerization of acetylene to 2-vinyloxy-1,3-butadiene in superbasic media takes place by a stepwise mechanism, involving the initial formation of acetaldehyde, its ethynylation, vinylation of the acetylenic alcohol, and prototropic acetyl-allene-1,3-diene rearrangements.A method was developed for the direct vinylation of primary and secondary acetylenic alcohols in the potassium hydroxide-DMSO system, leading to 3-vinyloxy-1-alkynes and 3-vinyloxy-1,2-alkadienes with overall yields of 45-87percent .
- Tarasova, O. A.,Trofimov, B. A.,Afonin, A. V.,Sinegovskaya, L. M.,Kalinina, N. A.,Amosova, S. V.
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p. 1018 - 1025
(2007/10/02)
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- Improved Procedure for the Asymmetric Reduction of Prochiral Ketones by B-(3-Pinanyl)-9-borabicyclononane
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An improved experimental procedure gives good optical induction in the reduction of nonacetylenic prochiral ketones, using the chiral trialkylborane B-(3-pinanyl)-9-borabicyclononane (Midland's reagent).
- Brown, Herbert C.,Pai, Ganesh G.
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p. 1606 - 1608
(2007/10/02)
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- Akenyl(or alkynyl) 9-xanthenyl ether compounds
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The compounds are alkenyl(and alkynyl) 9-xanthenyl ethers, for example allyl 9-xanthenyl ether, which are inhibitors of gastric acid secretion.
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