796851-05-3Relevant articles and documents
MANUFACTURE OF COMPOUNDS AND COMPOSITIONS FOR INHIBITING ACTIVITY OF SHP2
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Paragraph 00155; 00160-00161, (2022/02/06)
Provided herein is a method for the manufacture of a compound of Formula I or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme, wherein LG, A, n, m and p are as defined in the Summary of the Invention, said manufacture including the manufacture and use of a compound of the formula VI, wherein R1 is a secondary amino protecting group and R5 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl or unsubstituted or substituted aryl.
Aryl spiro compound containing formamidine as well as preparation method and application of aryl spiro compound
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Paragraph 0061-0064, (2021/08/14)
The invention belongs to the field of medicinal chemistry, and particularly relates to an aryl spiro compound containing formamidine as well as a preparation method and application of the aryl spiro compound. The invention relates to three aryl spiro compounds as shown in general formulas I-III and pharmaceutically acceptable salts, enantiomers, non-isomers, tautomers, solvates, polymorphic substances or prodrugs thereof. On the basis that SHP099 is used as a lead compound, a brand new compound with guanidyl at the tail end is prepared, and the problems that an existing SHP2 inhibitor is single in structural framework and the like are solved. The aryl spiro compound has the important significance of providing many modification sites and providing a basis for later structural modification. Meanwhile, the embodiment of the invention proves that the compound has an allosteric inhibition effect on SHP2 phosphatase, and a skeleton support is provided for subsequent development of an SHP2 phosphatase inhibitor.
MANUFACTURE OF COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2
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Paragraph 00237-00238, (2020/05/12)
The present invention relates to a method for the manufacture of a compound of Formula I or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme: wherein LG, A, n, m and p are as defined in the Summary of the Invention.
PROCESS OF MANUFACTURE OF A COMPOUND FOR INHIBITING THE ACTIVITY OF SHP2
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Paragraph 00308-00310; 00323; 00326, (2020/05/12)
The invention relates to a method for the manufacture of a compound of Formula I as mentioned above, or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II wit
Deprotonation of chloropyridines using lithium magnesates
Awad, Ha?an,Mongin, Florence,Trécourt, Fran?ois,Quéguiner, Guy,Marsais, Francis
, p. 7873 - 7877 (2007/10/03)
Chloropyridines are deprotonated using lithium magnesates. 4-Chloropyridine was deprotonated on treatment with 1/3 equiv of the highly coordinated magnesate Bu3(TMP)MgLi2 in THF at -10°C, as evidenced by trapping with I2. The use of Bu(TMP)2MgLi in Et 2O allowed the reaction of 2-chloropyridine, giving the 3-functionalized derivative as the main product. Mixtures of 3- and 4-functionalized derivatives were obtained when 2,6-dichloropyridine was involved in the reaction. Performing the reaction on 3-chloropyridine with lithium magnesates in THF, either the 4,4′-dimer or the 4-iodo derivative was formed after quenching by I2, the former using 1/3 equiv of Bu2(TMP)MgLi and the latter using 1 equiv of (TMP)3MgLi. Similar results were observed with 3,5-dichloropyridine, 2,5-dichloropyridine and 3-chloro-2-fluoropyridine. 1,2-Migration of the lithium arylmagnesate formed by deprotonation was proposed to justify the dimers formation.