The present invention relates to compounds of Formula (I):
that are have activity as S1P receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
Iron-Catalyzed Regiodivergent Hydrostannation of Alkynes: Intermediacy of Fe(IV)–H versus Fe(II)–Vinylidene
作者:Jianguo Liu、Heng Song、Tianlin Wang、Jiong Jia、Qing-Xiao Tong、Chen-Ho Tung、Wenguang Wang
DOI:10.1021/jacs.0c11448
日期:2021.1.13
iron-aryloxide catalyst (2, X = O-, R = Cy) affords an iron(II) vinylidene intermediate, allowing for gem-addition of the Sn-H to the terminal-carbon producing β-vinylstannanes. These catalytic reactions exhibit excellent regioselectivity and broad functional group compatibility and enable the large-scale synthesis of diverse vinylstannanes. Many new reactions have been established based on such a synthetic
我们报告了一种铁系统 Cp*Fe(1,2-R2PC6H4X),它通过调节离子金属-杂原子键 (Fe-X) 的反应性来控制炔烃的马尔科夫尼科夫和反马尔科夫尼科夫氢氢化。将 nBu3SnH 依次添加到铁-酰胺基催化剂 (1, X = HN-, R = Ph) 中提供了二锡基 Fe(IV)-H 物种,负责跨 C≡C 键的 Sn-H 键的顺式加成生产支链α-乙烯基锡烷。通过芳基氧化铁催化剂 (2, X = O-, R = Cy) 活化炔烃的 C(sp)-H 键,得到亚乙烯基铁 (II) 中间体,允许 Sn-H 与产生β-乙烯基锡烷的末端碳。这些催化反应表现出优异的区域选择性和广泛的官能团兼容性,能够大规模合成多种乙烯基锡烷。
Catalytic, Enantioselective Synthesis of Polycyclic Nitrogen, Oxygen, and Sulfur Heterocycles via Rh-Catalyzed Alkene Hydroacylation
作者:Kevin L. Vickerman、Levi M. Stanley
DOI:10.1021/acs.orglett.7b02230
日期:2017.10.6
Enantioselective synthesis of polycyclic nitrogen, oxygen, and sulfur heterocycles by rhodium-catalyzed intramolecular alkene hydroacylation is reported. The intramolecular hydroacylation reactions generate 1,4-dihydrocyclopenta[b]indol-3(2H)-ones and 3,4-dihydrocyclopenta[b]indol-1(2H)-one in moderate-to-high yields (65–99%) with good-to-excellent enantioselectivities (84–99% ee). The catalyst system
据报道,通过铑催化的分子内烯烃加氢酰化反应可对映选择性地合成多环氮,氧和硫杂环。分子内加氢酰化反应生成1,4-二氢环戊二烯并[ b ]吲哚-3-(2 ħ) -酮和3,4-二氢环戊二烯并[ b ]吲哚-1-(2- ħ) -酮在中度到高的产率(65-70 99%)具有良好至优异的对映选择性(84–99%ee)。该催化剂体系还促进3-乙烯基呋喃-,3-乙烯基苯并噻吩-和3-乙烯基噻吩-2-甲醛的烯烃加氢酰化反应,以中等至高的收率(71-91%的收率)产生相应的酮产物,并具有出色的对映选择性( 97–99%ee)。