- Acylazetine as a dienophile in bioorthogonal inverse electron-demand Diels-Alder ligation
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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.
- 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.
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supporting information
p. 2744 - 2747
(2014/06/09)
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- CARBOXAMIDE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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The invention relates to compounds of Formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
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Page/Page column 59-60
(2008/06/13)
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- Substituted triazole derivatives as oxytocin antagonists
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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.
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Page/Page column 21
(2008/06/13)
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- A practical and facile synthesis of azetidine derivatives for oral carbapenem, L-084
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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.
- Isoda, Takeshi,Yamamura, Itsuki,Tamai, Satoshi,Kumagai, Toshio,Nagao, Yoshimitsu
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p. 1408 - 1411
(2007/10/03)
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- Substituted benzoylpiperidine derivatives and their use as Neurokinin antagonists
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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.
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