36476-89-8Relevant academic research and scientific papers
Acylazetine as a dienophile in bioorthogonal inverse electron-demand Diels-Alder ligation
Engelsma, Sander B.,Willems, Lianne I.,Van Paaschen, Claudia E.,Van Kasteren, Sander I.,Van Der Marel, Gijsbert A.,Overkleeft, Herman S.,Filippov, Dmitri V.
supporting information, p. 2744 - 2747 (2014/06/09)
A new bioorthogonal N-acylazetine tag, suitable for tetrazine mediated inverse electron-demand Diels-Alder conjugation, is developed. The tag is small and achiral. We demonstrate the usefulness of N-acylazetine-tetrazine based bioorthogonal chemistry in two-step activity-based protein profiling. The performance of the new tetrazinophile in the labeling of catalytically active proteasome subunits was comparable to that of the more sterically demanding norbornene tag.
CARBOXAMIDE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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Page/Page column 59-60, (2008/06/13)
The invention relates to compounds of Formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
Substituted triazole derivatives as oxytocin antagonists
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Page/Page column 21, (2008/06/13)
The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
A practical and facile synthesis of azetidine derivatives for oral carbapenem, L-084
Isoda, Takeshi,Yamamura, Itsuki,Tamai, Satoshi,Kumagai, Toshio,Nagao, Yoshimitsu
, p. 1408 - 1411 (2007/10/03)
An orally active carbapenem L-084, which exhibits high bioavailability in humans, has a 1-(1,3-thiazolin-2-yl)azetidin-3-ylthio moiety at the C-2 position of the 1β-methylcarbapenem skeleton. We established a practical and cost-effective synthesis of 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine (1) for further scale-up production of L-084. This synthesis method entails an industry-oriented reaction of azetidine ring-closure to yield N-benzyl-3-hydroxyazetidine (16), which is eventually converted to 1 via key intermediates, Bunte salts 19 and 20.
Substituted benzoylpiperidine derivatives and their use as Neurokinin antagonists
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, (2008/06/13)
The present invention provides a compound of the formula:- or a pharmaceutically acceptable acid addition salt thereof, whereinAr is phenyl substituted by 1 or 2 substituent(s) each independently selected from fluoro and chloro;X is NSO2(C1-C4 alkyl), NSO2(halo(C1-C4 alkyl)) or O;m is 0 or 1 ;n is 1 or 2;p is 1 or 2;q is 1 or 2; and r is 1 or 2, together with processes for the preparation of, intermediates used in the preparation of, compositions containing and uses of, such derivatives. The compounds have tachykinin receptor antagonist activity.
