- (3+2)-Cycloaddition of Donor-Acceptor Cyclopropanes with Thiocyanate: A Facile and Efficient Synthesis of 2-Amino-4,5-dihydrothiophenes
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An easy and efficient route to obtain 2-amino-4,5-dihydrothiophenes is presented. A formal (3+2)-cycloaddition of donor-acceptor cyclopropanes and ammonium thiocyanate catalyzed by Yb(OTf) 3delivers the desired products in good to excellent yields. A broad range of functional groups is tolerated during this process.
- Jacob, Anu,Barkawitz, Philip,Andreev, Ivan A.,Ratmanova, Nina K.,Trushkov, Igor V.,Werz, Daniel B.
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supporting information
p. 901 - 904
(2021/03/17)
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- Method for synthesizing thiophenes inhibitor TPCA-1
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The invention relates to a method for synthesizing a thiophenes inhibitor TPCA-1, and belongs to the field of organic chemical drug synthesis. The method comprises the following steps: taking thioureaand 2-(4-fluorophenyl) cyclopropane-1,1-dimethyl isophthalate as starting raw materials, and the TPCA-1 is obtained through a multi-step reaction including a ring enlargement reaction, an oxidation reaction, an addition reaction and an amidation reaction in sequence. In the used route of the method, the reaction raw materials are easily obtained, the yield is high, and the TPCA-1 can be obtainedsuccessfully.
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Paragraph 0025-0029
(2019/04/02)
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- Thiourea participation in [3+2] cycloaddition with donor-acceptor cyclopropanes: A domino process to 2-amino-dihydrothiophenes
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The Yb(OTf)3-catalyzed [3+2] cycloaddition of donor-acceptor cyclopropanes with thiourea offers an efficient route to diverse 2-amino-4,5-dihydrothiophenes (up to 92% yield), in which optically active 2-amino-dihydrothiophenes can be produced f
- Xie, Ming-Sheng,Zhao, Guo-Feng,Qin, Tao,Suo, Yong-Bo,Qu, Gui-Rong,Guo, Hai-Ming
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supporting information
p. 1580 - 1583
(2019/02/07)
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- Gold(I)-Catalyzed 1,3-Carbofunctionalizations of Anthranils with Vinyl Propargyl Esters to Yield 1,3-Dihydrobenzo[ c]-isoxazoles
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This work describes gold-catalyzed 1,3-carbofunctionalizations of anthranils with vinyl propargyl esters to form 1,3-dihydrobenzo[c]-isoxazoles. Excellent diastereoselectivity has been achieved to yield products containing three stereogenic carbons. These
- Skaria, Manisha,Sharma, Pankaj,Liu, Rai-Shung
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supporting information
p. 2876 - 2879
(2019/04/30)
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- Synthesis of functionalized dihydrothiophenes from doubly activated cyclopropanes using tetrathiomolybdate as the sulfur transfer reagent
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A number of doubly activated cyclopropanes were synthesized starting from various substituted bromosulfonium bromides in good yield. Regioselective ring-opening of cyclopropanes with tetrathiomolybdate as the sulfur transfer reagent gave dihydrothiophenes
- Gopinath, Purushothaman,Chandrasekaran, Srinivasan
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supporting information; experimental part
p. 700 - 703
(2011/03/20)
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