- Preparation method 5,7 - dichloro -1, 2, 3 and 4 - tetrahydroisoquinoline
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The invention provides a preparation method of 5, 7 - dichloro -1, 2, 3 and 4 - tetrahydroisoquinoline, which comprises the following steps: reducing 2, 4 - dichlorobenzene acetonitrile by first reducing agent to generate 2 and 4 - dichlorophenylethylamin
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Paragraph 0058-0062
(2021/08/25)
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- Synthesis method of lifitegrast intermediate 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline
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The invention discloses a synthesis method of a lifitegrast intermediate 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline, wherein the synthesis method comprises the steps: by using 2,4-dichlorobenzaldehyde as a starting material, carrying out nitro-alcohol co
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Paragraph 0070-0073
(2020/05/05)
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- Synthesis and antioxidant characteristic of novel thiazolidinone derivatives
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A series of novel thiazolidinone derivatives have been synthesized by solventless condensation of N-alkylamines with arylaldehydes at room temperature followed by a microwave assisted solventless addition of thioglycollic acid to the resultant imines. The synthesized compounds are characterized by 1H NMR, 13C NMR, MS and X-ray techniques and one of the synthesized thiazolidinones has been evaluated for its antioxidant property.
- Amutha, Chinnadurai,Saravanan, Sivaperuman,Muthusubramanian, Shanmugam
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p. 377 - 383
(2014/05/06)
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- Activation of electrophilicity of stable Y-delocalized carbamate cations in intramolecular aromatic substitution reaction: Evidence for formation of diprotonated carbamates leading to generation of isocyanates
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Although cations with three heteroatoms, such as monoprotonated guanidine and urea, are stabilized by Y-shaped conjugation and such Y-conjugated cations are sufficiently basic to be further protonated (or protosolvated) to dications in strongly acid media, only O-monoprotonated species have been detected in the case of carbamates even in magic acid. We found that the trifluoromethanesulfonic acid-catalyzed cyclization of arylethylcarbamates proceeds to afford dihydroisoquinolones in high yield. In strong acids, methyl carbamates are fully O-monoprotonated, and these monocations do not undergo cyclization even under heating. But, as the acidity of the reaction medium is further increased, the cyclization reaction of methyl phenethylcarbamates starts to proceed as a first-order reaction, with a linear relationship between rate and acidity. The sign and magnitude of the entropy of activation ΔS ? were found to be similar to those of other AAc1 reactions. These results strongly support the idea that further protonation of the O-protonated carbamates is involved in the cyclization, but the concentration of the dications is very low and suggests that the rate-determining step is dissociation of methanol from the diprotonated carbamate to generate protonated isocyanate, which reacts with the aromatic ring. Therefore, O-protonated carbamates are weak bases in sharp contrast to other Y-shaped monocations.
- Kurouchi, Hiroaki,Kawamoto, Kyoko,Sugimoto, Hiromichi,Nakamura, Satoshi,Otani, Yuko,Ohwada, Tomohiko
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p. 9313 - 9328,16
(2012/12/11)
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- 2-aminobenzoxazole derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminobenzoxazole derivative compounds of the following formula: wherein R1 to R4 and Z have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminobenzoxazole derivative compounds.
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- 4-unsubstituted dihydroisoquinolinone derivatives and combinatorial libraries thereof
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The present invention relates to novel dihydroisoquinolinone (DHQ) derivative compounds of the following formula: wherein R1to R7, X, Y, Z, b, c and d have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing DHQ derivative compounds.
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