50419-88-0Relevant articles and documents
QUINOLINO-PYRROLIDIN-2-ONE DERIVATIVE AND APPLICATION THEREOF
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Paragraph 0076-0077; 0083-0084, (2021/07/08)
Disclosed are a series of quinolino-pyrrolidin-2-one compounds, and application thereof in preparation of drugs for ATM inhibitor-related diseases. The present disclosure specifically relates to a derivative compound represented by formula (I), tautomers thereof or pharmaceutically acceptable compositions thereof.
A 5 - bromo - 4 - chloro - 2 - amino preparation method of acetophenone (by machine translation)
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Paragraph 0019; 0020; 0028; 0029; 0036; 0037, (2017/08/29)
The invention discloses a 5 - bromo - 4 - chloro - 2 - amino acetophenone preparation method, the method comprises the following steps: to 4 - chloro - 2 - aminobenzoic acid as the starting material, the reaction of halide 5 - bromo - 4 - chloro - 2 - ami
Synthesis of DIBAC analogues with excellent SPAAC rate constants
Debets, Marjoke F.,Prins, Jasper S.,Merkx, Donny,Van Berkel, Sander S.,Van Delft, Floris L.,Van Hest, Jan C. M.,Rutjes, Floris P. J. T.
supporting information, p. 5031 - 5037 (2014/07/07)
In search for increased reactivity in strain-promoted azide alkyne cycloadditions (SPAAC), the synthesis of new and more reactive cyclooctynes is of pivotal importance. To identify cyclooctynes with enhanced reactivity, without loss of stability, the synthesis and kinetic analysis of new dibenzoazacyclooctyne (DIBAC) analogues were conducted. Starting from iodobenzyl alcohol analogues and ortho-ethynylaniline various substituted dihydrodibenzo[b,f]azocines were produced. Subsequent bromination and elimination proved to be difficult depending on the aromatic substitution pattern, yielding chloro-, bromo-, and methoxy-substituted DIBACs in moderate yield. In the elimination reaction towards nitro- and Br,Cl-DIBAC, the corresponding cyclooctene was obtained instead of the cyclooctyne. Additionally, a dimethoxy-substituted DIBAC analogue was prepared following an alternative route involving light-induced deprotection of a cyclopropenone derivative. In total, four DIBAC analogues were successfully prepared showing excellent rate constants in the SPAAC reaction ranging from 0.45 to 0.9 M-1 s -1, which makes them comparable to the fastest cyclooctynes currently known. This journal is the Partner Organisations 2014.