- Preparation method of (S)-(4-bromine-2-methylbenzene) (3-N-methylmorpholine) ketone
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The invention discloses a preparation method of (S)-(4-bromine-2-methylbenzene) (3-N-methylmorpholine) ketone, and belongs to the technical field of organic synthesis. The invention is characterized in that the preparation method of the (S)-(4-bromine-2-m
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Paragraph 0013; 0014; 0015
(2017/07/23)
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- NOVEL TRIAZINE COMPOUNDS
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The present invention relates to novel triazine compounds of formula (1). The present invention also discloses compounds of formula I along with other pharmaceutical ac-ceptable excipients and use of the compounds to modulate the PI3K/ mTOR pathway
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Page/Page column 126; 127
(2014/02/16)
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- A concise and efficient synthesis of substituted morpholines
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A simple and efficient method has been developed for the synthesis of substituted morpholines by a sequence of coupling, cyclization, and reduction reactions of easily available amino alcohols and α-halo acid chlorides. Various mono-, di-, and trisubstituted morpholines, spiro morpholines, and ring-fused morpholines, as well as morpholine homologues, were synthesized in good to excellent yields by a single methodology under similar reaction conditions. The method was also used in a multigram synthesis of (3S)-3-methylmorpholine.
- Dugar, Sundeep,Sharma, Amit,Kuila, Bilash,Mahajan, Dinesh,Dwivedi, Sandeep,Tripathi, Vinayak
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supporting information
(2015/02/19)
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- 2-AMINOBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS
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Compounds of formulae I, II and III: are disclosed as 5-HT3 inhibitors. The compounds are useful in treating CINV, IBS-D and other diseases and conditions.
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Page/Page column 17
(2008/12/04)
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- PYRAZOLE DERIVATIVE
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A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
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Page/Page column 147-148
(2010/11/27)
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- In vitro inhibition studies of phytoene desaturase by bleaching ketomorpholine derivatives
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The herbicidal activities of homochiral steroisomeric 5-methyl-2-(3-trifluoromethylbenzyl)-3-ketomorpholine derivatives were investigated in vitro as inhibitors of phytoene desaturase, a key enzyme in carotenoid biosynthesis. It was demonstrated that ketomorpholines are classical bleaching compounds which directly inhibit phytoene desaturase, accumulating phytoene at the expense of colored carotenoids. Ketomorpholines interact with phytoene desaturase in a noncompetitive manner with respect to phytoene. A structure-activity investigation for in vitro inhibition of phytoene desaturase activity revealed that the relative and absolute stereochemistry is important for optimum inhibition for the 5-methyl derivatives, and that the distance of the phenyl group from the ketomorpholine ring is critical for the inhibitory potential. The average herbicidal score on 7 weeds and the in vitro I50 values related very well with the exception of two compounds. It was postulated that the discrepancies may possibly occur through modification in plants to compounds that are either more or less active herbicides.
- Sandmann, Gerhard,Mitchell, Glynn
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p. 138 - 141
(2007/10/03)
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- Alkylation studies of N-protected-5-substituted morpholin-3-ones. A stereoselective approach to novel methylene ether dipeptide isosteres
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We have developed a versatile new synthesis of the Ψ[CH2O] pseudopeptides from N-protected-5-substituted morpholin-3-ones. The morpholin-3-ones are prepared in two steps from the corresponding amino alcohols by treatment with ethyl chloroacetate, followed by protection of the amide. We found that direct alkylation of the protected morpholin-3-ones gives the expected alkylation product where the electrophile approaches from the face opposite to the existing side chain (derived from the amino alcohol). If an S amino alcohol is used, this procedure results in the formation of the (S,R) Ψ[CH2O] dipeptide. Alternatively, the (S,S) Ψ[CH2O] dipeptide can be obtained if the protected morpholin-3-one enolate is quenched with an aldehyde and the aldol product is dehydrated and reduced. We have explored an alkylation/deprotonation/kinetic protonation scheme which is also amenable to the preparation of (S,S) pseudodipetides. It is, of course, possible to obtain the corresponding (R,R) and (S,R) Ψ[CH2C] dipeptides by simply selecting the appropriate amino alcohols and reaction conditions. Finally, we have established that this method is general and can be applied to the preparation of numerous Ψ[CH2C] dipeptides which were previously unavailable by existing methods.
- Norman, Bryan H.,Kroin, Julian S.
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p. 4990 - 4998
(2007/10/03)
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