公开(公告)号：US08871916B2

公开(公告)日：2014-10-28

申请号：US13715842

申请日：2012-12-14

Applicant: Ronald Thaddeus Raines ,  Eddie Leonard Myers

Inventor： Ronald Thaddeus Raines ,  Eddie Leonard Myers

IPC: C07F9/32 ,  C07C247/12 ,  C07C271/22 ,  C07F9/50 ,  C07F9/53 ,  C07F9/572 ,  C07C247/10 ,  C07F9/28 ,  C07C247/14 ,  C07C245/12 ,  C07C245/18 ,  C07D223/16 ,  C07C251/00

CPC classification number: C07C245/18 ,  C07C245/12 ,  C07C247/10 ,  C07C247/12 ,  C07C247/14 ,  C07C251/00 ,  C07C271/22 ,  C07C2601/14 ,  C07C2603/18 ,  C07C2603/24 ,  C07D223/16 ,  C07F9/28 ,  C07F9/5022 ,  C07F9/5325 ,  C07F9/572

Abstract: A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diazo-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compounds and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.

Abstract translation: 制备重氮化合物，其重氮盐和这些化合物的其它保护形式的方法。 重氮化合物是通过将载有反应性羰基的叔膦试剂与叠氮化物反应来制备的。 反应也可以产生酰基三氮烯，其可以热转化或加入碱形成重氮化合物，或者可以分离酰基三氮烯。 该方法对于携带一个或多个吸电子基团的叠氮化物转化为重氮化合物是特别有用的。 该方法可以在温和条件下在水性介质中进行，特别适用于在生理条件下将叠氮基糖转化为重氮化合物和重氮盐。 提供了叔膦试剂，特别是水溶性试剂，以及制备试剂的前体。

公开(公告)号：US08350014B2

公开(公告)日：2013-01-08

申请号：US12620567

申请日：2009-11-17

Applicant: Ronald Thaddeus Raines ,  Eddie Leonard Myers

Inventor： Ronald Thaddeus Raines ,  Eddie Leonard Myers

IPC: C07C245/14 ,  C07C245/20 ,  C07C245/24

CPC classification number: C07C245/18 ,  C07C245/12 ,  C07C247/10 ,  C07C247/12 ,  C07C247/14 ,  C07C251/00 ,  C07C271/22 ,  C07C2601/14 ,  C07C2603/18 ,  C07C2603/24 ,  C07D223/16 ,  C07F9/28 ,  C07F9/5022 ,  C07F9/5325 ,  C07F9/572

Abstract: A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.

Abstract translation: 制备重氮化合物，其重氮盐和这些化合物的其它保护形式的方法。 通过使带有反应性羰基的叔膦试剂与叠氮化物反应来制备二嗪化合物。 反应也可以产生酰基三氮烯，其可以热转化或加入碱形成重氮化合物，或者可以分离酰基三氮烯。 该方法对于携带一个或多个吸电子基团的叠氮化物转化为重氮化合物是特别有用的。 该方法可以在温和条件下在水性介质中进行，特别适用于在生理条件下将叠氮基糖转化为重氮化合物和重氮盐。 提供了叔膦试剂，特别是水溶性试剂，以及制备试剂的前体。

公开(公告)号：US20100125132A1

公开(公告)日：2010-05-20

申请号：US12620567

申请日：2009-11-17

Applicant: Ronald Thaddeus Raines ,  Eddie Leonard Myers

Inventor： Ronald Thaddeus Raines ,  Eddie Leonard Myers

IPC: C07C245/18 ,  C07F9/50 ,  C07C69/767 ,  C07F9/28

CPC classification number: C07C245/18 ,  C07C245/12 ,  C07C247/10 ,  C07C247/12 ,  C07C247/14 ,  C07C251/00 ,  C07C271/22 ,  C07C2601/14 ,  C07C2603/18 ,  C07C2603/24 ,  C07D223/16 ,  C07F9/28 ,  C07F9/5022 ,  C07F9/5325 ,  C07F9/572

Abstract: A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.

Abstract translation: 制备重氮化合物，其重氮盐和这些化合物的其它保护形式的方法。 通过使带有反应性羰基的叔膦试剂与叠氮化物反应来制备二嗪化合物。 反应也可以产生酰基三氮烯，其可以热转化或加入碱形成重氮化合物，或者可以分离酰基三氮烯。 该方法对于携带一个或多个吸电子基团的叠氮化物转化为重氮化合物是特别有用的。 该方法可以在温和条件下在水性介质中进行，特别适用于在生理条件下将叠氮基糖转化为重氮化合物和重氮盐。 提供了叔膦试剂，特别是水溶性试剂，以及制备试剂的前体。