有机二硫化物代表了化学生物学、制药领域和工业中丰富的一类化合物。它们传统上是通过在有机配体负载的金属催化剂或有毒氧化剂的存在下在恶劣条件下氧化硫醇来合成的。在这里,我们公开了一种高效途径,其中使用催化剂 (NH 4 ) 3 [CrMo 6 O 18 (OH) 6由有机硼酸和 Na 2 S 2 O 3合成二硫化物],显示出高活性和出色的选择性。各种硼酸衍生物已成功转化为相应的二硫化物。基于对中间和控制实验的观察提供了机械见解。
Thiochromane derivatives and their use as thrombin inhibitors
申请人:——
公开号:US20030220317A1
公开(公告)日:2003-11-27
There is provided compounds of formulae I and IA
1
wherein Y, R
1
, R
2
, R
3
, D
1
and D
2
have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
NEW THIOCHROMANE DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS
申请人:AstraZeneca AB
公开号:EP1283837B1
公开(公告)日:2004-02-25
US6716834B2
申请人:——
公开号:US6716834B2
公开(公告)日:2004-04-06
[EN] NEW THIOCHROMANE DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS<br/>[FR] NOUVEAUX DERIVES DE THIOCHROMANE ET LEUR UTILISATION COMME INHIBITEURS DE THROMBINE
申请人:ASTRAZENECA AB
公开号:WO2001087879A1
公开(公告)日:2001-11-22
There is provided compounds of formulae (I) and (IA) wherein Y, R?1, R2, R3, D1 and D2¿ have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of trypsinlike proteases, such as thrombin, and in particular in the treatment of conditions where inhibitors of thrombin is required (e.g. thrombosis) or as anticoagulants.
Transformation of arylboronic acids with sodium thiosulfate into organodisulfides catalyzed by a recyclable polyoxometalate-based Cr(<scp>iii</scp>) catalyst
toxic oxidants under harsh conditions. Here, we disclose a highly-efficient pathway in which disulfide is synthesized by organic boric acid and Na2S2O3 using the catalyst (NH4)3[CrMo6O18(OH)6], demonstrating a high activity and excellent selectivity. Various boric acid derivatives have been successfully transformed into the corresponding disulfides. Mechanistic insights have been furnished based on the
有机二硫化物代表了化学生物学、制药领域和工业中丰富的一类化合物。它们传统上是通过在有机配体负载的金属催化剂或有毒氧化剂的存在下在恶劣条件下氧化硫醇来合成的。在这里,我们公开了一种高效途径,其中使用催化剂 (NH 4 ) 3 [CrMo 6 O 18 (OH) 6由有机硼酸和 Na 2 S 2 O 3合成二硫化物],显示出高活性和出色的选择性。各种硼酸衍生物已成功转化为相应的二硫化物。基于对中间和控制实验的观察提供了机械见解。