105706-75-0Relevant articles and documents
The Synthesis of 1-Methyl-6,7,8,8a-tetrahydro-5H-indolizin-3-one by the Palladium-Catalyzed Cyclization of N-Bromoacetyl-2-vinylpiperidine
Yang, Shyh-Chyun,Shea, Fang-Rong,Chung, Wen-Hung
, p. 293 - 296 (1998)
N-Bromoacetyl-2-vinylpiperidine underwent cyclizalion to give indolizidine derivative in the presence of a base and a catalytic amount of palladium trifluoroacetate.
Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist
Betz, Stephen F.,Chen, Zhiyong,Kusnetzow, Ana Karin,Nguyen, Julie,Rico-Bautista, Elizabeth,Struthers, R. Scott,Tan, Hannah,Zhao, Jian,Zhu, Yunfei
, (2020)
The discovery of a novel 3H-pyrido[2,3-d]pyrimidin-4-one series as potent and biased sst2 agonists is described. This class of molecules exhibits excellent sst2 potency and selectivity against sst1, sst3, and sst5 receptors, and they are significantly more potent at inhibiting cAMP production than inducing internalization. The orally bioavailable 6-(3-chloro-5-methylphenyl)-3-(3-fluoro-5-hydroxyphenyl)-5-({methyl[(2S)-pyrrolidin-2-ylmethyl]amino}methyl)-3H,4H-pyrido[2,3-d]pyrimidin-4-one (36) also suppresses GH secretion in GHRH-challenged rats in a dose-dependent manner.
Pyrrolidinic and piperidinic ring fission by conjugate elimination
Acquadro, Francesco,Oulyadi, Hassan,Venturello, Paolo,Maddaluno, Jacques
, p. 8759 - 8763 (2002)
Treating N-substituted pyrrolidines and piperidines bearing an allylic chain α to the nitrogen with strong bases leads to the opening of the heterocycle and provides 1,3-dienes disubstituted with an alkoxy and an aminoalkyl chain. The effects of the base and the solvent have been studied, as well as the influence of the ring size and the nitrogen substituent. The results obtained suggest a possible pre-chelation of the base cation before the deprotonation.
A library of conformationally restricted saturated heterocyclic sulfonyl chlorides
Zhersh, Sergey,Buryanov, Volodymyr V.,Karpenko, Oleksandr V.,Grygorenko, Oleksandr O.,Tolmachev, Andrey A.
scheme or table, p. 3669 - 3674 (2011/12/16)
An approach to the synthesis of conformationally restricted saturated heterocyclic sulfonyl chlorides is described. Being guided by the principle of diversity-oriented conformational restriction, a mini-library of saturated heterocyclic sulfonyl chlorides
NEW BRADYKININ B1 ANTAGONISTS
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, (2008/12/08)
The invention relates to compounds of formula (I), wherein R1 to R5 and X1 to X4, n and m have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The
Microwave-assisted carbamoylation of amines
Azzena, Ugo,Dettori, Giovanna,Pisano, Luisa,Pittalis, Mario
, p. 3623 - 3634 (2008/03/13)
The influence of microwave irradiation on the reaction of various amines with benzyl chloroformate and di-tert-butyl dicarbonate was investigated. Microwave irradiation was successfully applied to the carbamoylation of several nonfunctionalized and functionalized amines, including amino acids and nucleobases, leading to satisfactory to high product conversion within very short reaction times. Copyright Taylor & Francis Group, LLC.
FUSED BENZENE DERIVATIVE AND USE
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Page/Page column 38, (2010/02/12)
The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3' (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5' (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively. The formula represents a single bond or a double bond] or a salt thereof, which is useful as an androgen receptor modulator.
Src kinase inhibitor compounds
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, (2008/06/13)
Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
Short syntheses of (S)-pipecolic acid, (R)-coniine, and (S)-δ-coniceine using biocatalytically-generated chiral building blocks
Sanchez-Sancho, Francisco,Herradon, Bernardo
, p. 1951 - 1965 (2007/10/03)
The kinetic resolutions of both (±)-N-(benzyloxycarbonyl-2- (hydroxymethyl)piperidine [(±)-5] and (±)-N(tert-butoxycarbonyl)-2- (hydroxymethyl)piperidine [(±)-6] catalyzed by the enzyme acylase I from Aspergillus species (AA-I) afforded the chiral building blocks (S)-5 and (S)- 6, respectively; which were used for the syntheses of the title natural products and derivatives of (S)-pipecolic acid. The syntheses were short (2- 4 steps) and proceeded with satisfactory overall yield.
DERIVATIVES OF HETEROCYCLIC α-IMINOCARBOXYLIC ACIDS. 4. REDUCTION OF N-ALKOXYCARBONYL DERIVATIVES OF α-IMINOCARBOXYLIC ACIDS.
Nurdinov, R.,Liepin'sh, E. E.,Kalvin'sh, I. Ya.
, p. 1352 - 1357 (2007/10/02)
When N-methoxycarbonyl and N-benzoxycarbonyl derivatives of methyl esters of aziridine-2-carboxylic acid, L-proline, L-thioproline, and pipecolic acid interact with NaBH4 in tert-butanol/methanol, the products of reduction of the C-methoxycarbonyl group o
