One-Pot Synthesis of Alkoxyamine Derivatives by Reductive Alkoxyamination with a 2-Picoline-Borane Complex
摘要:
Reduction of oxime ethers with a 2-picoline-borane complex was examined to give alkoxyamine derivatives. The reduction was found to proceed in the presence of aqueous HCl in MeOH-AcOH. The method was extended to one-pot synthesis of alkoxyamine derivatives from aldehydes and ketones. The reaction of carbonyl compounds with alkoxyamines in MeOH-AcOH (10:1), followed by sequential treatment with 2-picoline-borane and 3M HCl afforded alkoxyamine derivatives in good yields. This procedure can be applied to the synthesis of various alkoxyamine derivatives from aliphatic/aromatic aldehydes and ketones.
The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof:
1
wherein R
1
, R
2
and B
1
are as defined herein.
The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds.
1
TAM FAMILY KINASE /AND CSF1R KINASE INHIBITOR AND USE THEREOF
申请人:Nanjing Transthera Biosciences Co., Ltd.
公开号:US20210177828A1
公开(公告)日:2021-06-17
The present invention provides a novel inhibitor compound of general formula (I), exhibiting excellent kinase inhibitor activity. The compound of the present invention can be used to prevent and/or treat diseases mediated by abnormal expression of TAM family kinase receptors and/or ligands thereof. In addition, the compound of the present invention can also target CSF1R kinase, and thus can be used to prevent and/or treat diseases mediated by abnormal expression of TAM family kinase receptors and/or CSF1R kinase receptors and/or ligands thereof.
HYDROGENATION PROCESS OF OXIME DERIVATIVES
申请人:SYNGENTA CROP PROTECTION AG
公开号:US20210387173A1
公开(公告)日:2021-12-16
The present invention relates to a novel process for the iridium-catalysed hydrogenation of oximes. The invention also relates to novel iridium catalysts for use in the iridium-catalysed hydrogenation of oximes and to processes of preparation of these catalysts. The invention further relates to the use of the novel iridium catalysts in ionic hydrogenation of other unsaturated substrates.