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.
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.
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.