- Palladium-Catalyzed Dehydrogenative Difunctionalization of Aminoalkenes with Aminals as Oxidants and Electrophiles
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A novel palladium-catalyzed aminomethylamination of aminoalkenes with an aminal, functioning not only as an aminomethylation reagent but also as an oxidant, was developed. This direct and operationally simple protocol provides a fundamentally novel and unique approach toward the synthesis of 2-(2-aminoethyl)indoles and 2-(2-aminoethyl)pyrrolidines, which are important building blocks in synthetic organic chemistry. The unity of this method was highlighted by the rapid synthesis of Alosetron, a drug used for the treatment of irritable bowel syndrome.
- Li, Lixin,Zhou, Xibing,Yu, Bangkui,Huang, Hanmin
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supporting information
p. 4600 - 4603
(2017/09/12)
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- Cyclic Anti-Azacarboxylation of 2-Alkynylanilines with Carbon Dioxide
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Direct anti-azacarboxylation of 2-alkynylanilines with CO2 mediated by ZnEt2 was observed to afford indole-3-carboxylic acids, a class of important compounds for the synthesis of many biologically active compounds, efficiently under 1 atm of CO2. The readily available nature of the different starting materials and tolerance of various functional groups provide vast opportunities for the efficient construction of diversified libraries for bioactive compounds listed in Figure 1. As an example, this methodology has been applied to the synthesis of Lotronex, a drug molecule used for the treatment of irritable bowel syndrome.
- Miao, Bukeyan,Li, Suhua,Li, Gen,Ma, Shengming
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supporting information
p. 2556 - 2559
(2016/07/06)
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- INDOLONE MODULATORS OF 5-HT3 RECEPTOR
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The present invention relates to new indolone modulators of 5-HT3 receptor, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 12
(2010/05/13)
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- PROCESS FOR THE PREPARATION OF LACTAM DERIVATIVES
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The invention relates to a process for the preparation of a compound of formula (I) STR1 wherein R represent a hydrogen atom or a methyl or ethyl group, which comprises cyclising a compound of formul (IV) STR2 Where R represents a hydrogen atom, the compound of formula (IV) may optionally be alkylated to produce a compound in whcich R is methyl or ethyl.The compound of formula (I) is useful as an intermediate in the preparation of 2,3,4,5-tetrahydro-2-[(imidazol-4(or 5)-yl)methyl]-1H-pyrido[4,3-b]indol-1-ones having 5-HT 3 antagonist activity.
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