A Facile Approach to the Synthesis of 3-(6-Chloro-thiazolo[5,4-b]pyridin-2-ylmethoxy)-2,6-difluoro-benzamide (PC190723)
摘要:
Practical synthesis of PC 190723, a bacterial cell division protein Ftsz inhibitor, has been achieved in a high overall yield of 45% in six steps from commercially available starting materials.
preparation in THF, a heterogeneous mixture developed and centrifugation of the suspension allowed for separation of the precipitate, which contained the active catalyst and which could be stored for at least 1 month without any loss of catalytic performance. The precipitate promoted a nitroaldol (Henry) reaction for a broad range of nitroalkanes and aldehydes under heterogeneous conditions, affording
描述了由 Nd(5)O(O(i)Pr)(13)、基于酰胺的配体和 NaHMDS(六甲基二硅肼钠)组成的异双金属催化剂促进的抗选择性催化不对称硝基醛醇反应的全部细节。酰胺基配体的系统合成和评估导致最佳配体1m的鉴定,这为Nd/Na异质双金属配合物提供了合适的平台。在 THF 中制备催化剂的过程中,形成了一种非均相混合物,悬浮液的离心允许沉淀物分离,其中含有活性催化剂并且可以储存至少 1 个月而不会损失任何催化性能。沉淀促进了多种硝基烷烃和醛在非均相条件下的硝基醛醇 (Henry) 反应,得到相应的 1, 2-硝基烷醇以高度抗选择性(高达 anti/syn = >40/1)和对映选择性方式(高达 98% ee)。电感耦合等离子体 (ICP) 和 X 射线荧光 (XRF) 分析表明,沉淀确实包含钕和钠,高分辨率 ESI TOF MS 光谱法进一步支持了这一点。
P38 MAP kinase inhibitors
申请人:RespiVert Ltd.
公开号:US08299074B2
公开(公告)日:2012-10-30
The present disclosure relates to compounds of formula (I):
which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
The present disclosure relates to compounds of formula (I):
which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD