- Diphenylsilane as a coupling reagent for amide bond formation
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A simple procedure for amide bond formation using diphenylsilane as a coupling reagent is described. This methodology enables the direct coupling of carboxylic acids with primary and secondary amines, releasing only hydrogen and a siloxane as by-products. Only one equivalent of each partner is needed, providing a more sustainable amidation method producing minimal wastes. This methodology was also extended to the synthesis of peptides and lactams by addition of Hünig's base (DIPEA) and 4-dimethylaminopyridine (DMAP).
- Sayes, Morgane,Charette, André B.
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supporting information
p. 5060 - 5064
(2017/11/09)
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- Total synthesis of padanamides A and B
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The first total syntheses of padanamides A and B have been achieved, unambiguously confirming their structures. The Royal Society of Chemistry.
- Long, Bohua,Tang, Shoubin,Chen, Ligong,Qu, Shiwei,Chen, Bo,Liu, Junyang,Maguire, Anita R.,Wang, Zhuo,Liu, Yuqing,Zhang, Hui,Xu, Zhengshuang,Ye, Tao
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p. 2977 - 2979
(2013/05/22)
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- Synthesis and biological activity of sulphostin analogues, novel dipeptidyl peptidase IV inhibitors
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The structure of sulphostin (1), a novel dipeptidyl peptidase IV (DPP-IV) inhibitor, is consisted of three key functional groups, including a characteristic amino(sulfoamino)phosphinyl group, on a piperidine ring. To examine the relationship between its s
- Abe, Masatoshi,Akiyama, Tetsuo,Umezawa, Yoji,Yamamoto, Keiichiro,Nagai, Masashi,Yamazaki, Hiroko,Ichikawa, Yuh-Ichiro,Muraoka, Yasuhiko
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p. 785 - 797
(2007/10/03)
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- A flexible approach to (S)-3-amino-2-pyrrolidinone derivatives
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Starting from (S)-aspartic acid, a flexible chemoselective approach to (S)-3-amino-2-pyrrolidinone derivatives was reported. The (S)-3-amino-2-pyrrolidinone derivatives thus synthesized are useful templates for designing medicinal interesting compounds.
- Tang, Tian,Zhu, Chen,Huang, Pei-Qiang
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p. 121 - 128
(2007/10/03)
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- Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
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The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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Page/Page column 41
(2008/06/13)
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- Sulphostin analogue and process for producing sulphostin and its analogue
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A sulphostin analogue represented by the general formula, wherein n is an integer of from 0 to 3, provided that a case where n is 2 and steric configurations of C* and P* are S and R, respectively, is excluded, or a pharmaceutically acceptable salt thereof.
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- Azacycloalkanone serine protease inhibitors
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The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compoun
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- Synthesis and in vitro enzyme activity of aza, oxa and thia derivatives of bacterial cell wall biosynthesis intermediates
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Mechanism based inhibitors of diaminopimelate aminotransferase (DAP-AT) were designed using knowledge of its substrate specificity and mechanism. Synthesis of thiolester and amide substrate analogues was achieved prior to in vitro inhibition studies, but ester analogues proved too unstable to isolate. Thia substrate analogues showed no inhibitory properties, but the aza substrate analogue 12a showed reversible inhibition vs. DAP-AT and time dependent inhibition in the absence of the natural substrate 4. Substrate analogue 12a is thefirst example of an amide inhibitor of PLP dependent enzymes. Antibiotic properties of 12a were also briefly assessed.
- Cox,Wang
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p. 2022 - 2034
(2007/10/03)
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- SPONTANEOUS CYCLIZATION OF A CHAIN SHORTENED LYSINE ANALOG
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The chain shortened analog of lysine, H2NCH2CH2CH(NHZ)COOR, generated from N-protected glutamine esters, undergoes spontaneous cyclization.The results show that amino acids having H2NCH2CH2 - side chains cannot be supported on tRNA and provides a rationale for keeping the amino group of lysine by as many as four methylenes away from the peptide backbone.In sharp contrast, in the peptide environment, H2NCH2CH2CH(NHZ)CONHCH(X)COOMe, this unit is stable, thus demonstrating that if they are post translationally created, can be present as viable side chains in proteins.
- Ranganathan, S.,Ranganathan, D.,Singh, W. P.
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p. 3111 - 3114
(2007/10/02)
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