CAS: 243984-11-4; (R)-Ethyl 6-(N-(2-Chloro-4-Fluorophenyl)Sulfamoyl)Cyclohex-1-Enecarboxylate

上下游产品

CAS号340722-43-2 (6RS)-6-[N-(2-c... | CAS号243983-70-2 6-(N-(2-氯-4-氟苯基... | CAS号54928-91-5 2-疏基环己烯-1-羧酸乙酯 | CAS号1655-07-8 2-环己酮甲酸乙酯 | CAS号243984-26-1 2-(氯磺酰基)环己烯-1-羧酸乙酯 | CAS号243984-25-0 2-(ethoxycarbon... | CAS号64-17-5 乙醇 | CAS号340722-42-1 acetoxymethyl (...

📜(6Rs)-6-[n-(2-Chloro-4-Fluorophenyl)Sulfamoyl]Cyclohex-1-Ene-1-Carboxylic Acid置于lipase Ps-D,硫酸,四丁基碘化铵,Caesium Carbonate体系中,用 水,丙酮,乙腈 用作溶剂,化学反应 45.0H,反应生成瑞沙托维
参考文献:光学活性环己烯衍生物作为一种新型防腐剂:乙基(6R)-6-[n-(n-(2-氯-4-氟苯基)氨磺酰基]环己-1-烯-1-羧酸(tak-242)的有效合成.
标题:光学活性环己烯衍生物作为一种新型防腐剂:乙基(6R)-6-[n-(n-(2-氯-4-氟苯基)氨磺酰基]环己-1-烯-1-羧酸(tak-242)的有效合成.
摘要:建立了两种新的合成方法,可有效合成光学活性的环己烯防腐剂,乙基(6R)-6-[n-(n-(2-氯-4-氟苯基)氨磺酰基]环己-1-烯-1-羧酸[[r )-1:Tak-242)].第一种方法涉及通过将羧酸3与(S)-1-(4-硝基苯基)乙醇[(S)-5)酯化获得的非对映混合物(6Rs,1'R)-7从甲醇中重结晶为得到具有99%de的所需异构体(6R,1'R)-7,产率为32%.随后的催化氢解和酯化得到具有> 99%ee的(R)-1.第二种方法是使用脂酶ps-D对乙酰氧基甲酯9A(通过3与溴乙酸甲酯的烷基化反应)进行对映选择性水解,从而得到对映体对映异构体(R)-9A,具有优异的对映选择性(> 99%ee)和高收率(48%) ).然后通过在浓硫酸存在下与乙醇进行酯交换而获得所需的(R)-1,而不会损失ee.其中,使用脂肪酶ps-D进行酶促动力学拆分的方法是(R)-1的更有效和实用的制备方法.
Doi:10.1248/cpb.54.58

专利信息

专利号:US-10370455-B2
优先权日:2014-12-05
标题 :Identification of VSIG8 as the putative VISTA receptor (V-R) and use thereof to produce VISTA/VSIG8 agonists and antagonists
发明人：MOLLOY MICHAEL; GUO YALIN; ROTHSTEIN JAY; ROSENZWEIG MICHAEL
权利人:IMMUNEXT INC
摘要:The receptor for VISTA is identified (VSIG8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG8 and/or VISTA and/or the VSIG8/VISTA binding interaction. These antagonists may be used to suppress VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

专利号:US-6982344-B2
优先权日:2000-10-18
标 题:Process for preparation of optically active sulfonamides and intermediates for their synthesis
发明人：IKEMOTO TOMOMI; NISHIGUCHI ATSUKO; TOMIMATSU KIMINORI
权利人:TAKEDA PHARMACEUTICAL
摘要:A method including resolution of a diastereomeric mixture represented by the formula n n nwherein R 1 and R 2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, only one of R 1 and R 2 contains one asymmetric carbon, and R a is an optically active and optionally substituted hydrocarbon group or an optically active and optionally substituted heterocyclic group, or a salt thereof, to produce the diastereomer having a steric configuration of the asymmetric carbon for R 1 or R 2 of an R configuration or an S configuration, or a salt thereof.

专利号:US-2004049041-A1
优先权日:2000-10-18
标 题 :Process for preparation of optically active sulfonamides and intermediates for their synthesis

专利号:CA-2426277-C
优先权日:2000-10-18
标题 :Process for preparation of optically active sulfonamides and intermediates for their synthesis

专利号:EP-1334966-B1
优先权日:2000-10-18
标题:Process for preparation of optically active sulfonamides and intermediates for their synthesis

专利号:EP-1334966-A1
优先权日:2000-10-18
标 题 :Process for preparation of optically active sulfonamides and intermediates for their synthesis