137618-52-1Relevant academic research and scientific papers
MORPHOLINE AND 1,4-OXAZEPANE AMIDES AS SOMATOSTATIN RECEPTOR SUBTYPE 4 (SSTR4) AGONISTS
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Page/Page column 88, (2016/06/06)
The invention relates to morpholine and 1,4-oxazepane amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention
Synthesis of 4-substituted 3,3-difluoropiperidines
Surmont, Riccardo,Verniest, Guido,Thuring, Jan Willem,Macdonald, Gregor,Deroose, Frederik,De Kimpe, Norbert
supporting information; experimental part, p. 929 - 932 (2010/07/02)
Synthetic strategies toward 4-substituted 3,3-difluoropiperidines were evaluated. 4-Alkoxymethyl- and 4-aryloxymethyl-3,3-difluoropiperidines were synthesized via 1,4-addition of ethyl bromodifluoroacetate to 3-substituted acrylonitriles in the presence o
Efficient lipase-catalyzed kinetic resolution of 4-arylmethoxy-3-hydroxybutanenitriles: application to an expedient synthesis of a statin intermediate
Sun, Fenglai,Xu, Gang,Wu, Jianping,Yang, Lirong
, p. 2907 - 2913 (2007/10/03)
The kinetic resolution of 4-arylmethoxy-3-hydroxybutanenitriles was investigated by lipase-catalyzed transesterification in organic solvents. A high enantioselectivity was obtained via reaction with vinyl acetate in a mixed solvent (n-heptane/acetonitrile 1:1), which was catalyzed by the lipase from Artgribacter sp. A better selectivity was demonstrated when the number of substituents on the aryl ring increased. (S)-4-Arylmethoxy-3-hydroxybutanenitriles can be obtained with enantiomeric excesses of up to 98.0% by this method. Furthermore we have developed a novel route to synthesize tert-butyl (S)-6-benzyloxy-5-hydroxy-3-oxohexanoate, a key intermediate for the preparation of HMG-CoA reductase inhibitors (statins).
Pyrimidine derivatives
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, (2008/06/13)
Pyrimidine derivatives useful as a gastrointestinal prokinetic agent, represented by formula STR1 wherein X is O or NR5, Y is O, S or NR5 wherein R5 is a hydrogen atom, a C1 -C6 alkyl group or the like; R1 and R2 may be the same or different and each is a hydrogen atom, a C1 -C6 alkyl group or the like; R3 is CN, or COOR6 wherein R6 is a C1 -C6 alkyl group, a C3 -C6 cycloalkyl group, an aryl group or the like; R4 is --SR7 or --NR8 R9 wherein R7 is a C1 -C6 alkyl group; R8 is a C1 -C6 alkyl group or the like; R9 is a hydrogen atom, a C1 -C6 alkyl group or the like, or R8 and R9 may represent, together with the nitrogen atom to which they are attached, an N-substituted piperazine ring of formula (X) STR2 wherein R10 represents a C1 -C6 alkyl group or the like or a pharmacologically acceptable salt thereof. The above-mentioned compounds are useful as a gastrointestinal prokinetic agent used for the therapy of digestive tract diseases.
Nucleophilic Addition to Cyclic 1,2-Sulfites
Carlsen, Per H.,Aase, Kristin J.
, p. 617 - 619 (2007/10/02)
Addition of heteroatom nucleophiles has been shown to attack at either the C5- or the S-atom sites in 4-(benzyloxymethyl)-1,3-dioxa-2-thiolane 2-oxide.No C4-reactivity was observed.The regioselectivity depended on the type of nucleophile.
Selective monoalkylation of acyclic diols by means of dibutyltin oxide and fluoride salts
Nagashima,Ohno
, p. 1972 - 1982 (2007/10/02)
Fluoride anion was found to promote monoalkylation reaction of diols by the stannylene acetal method, and selective monoalkylation of various acyclic diols was accomplished in good yields under mild conditions by employing this new method. Functional groups such as carboxylic acid ester, carboxamide, carbamate, nitrile, alkyl chloride, and ether were not affected under the reaction conditions.
