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1. 发明申请

US20070276145A1 Method of Preparing a Ring Compound Having Two Adjacent Chiral Centers 审中-公开
标题翻译：制备具有两个相邻手性中心的环化合物的方法
公开(公告)号：US20070276145A1
公开(公告)日：2007-11-29
申请号：US10554135
申请日：2004-04-19
申请人： Lisa Schultze , John Demattei , Brad Barnett , Anthony Piscopio , Paul Nichols
发明人： Lisa Schultze , John Demattei , Brad Barnett , Anthony Piscopio , Paul Nichols
IPC分类号： C07D207/16 , C07C201/12
CPC分类号： C07D207/277 , C07C201/12 , C07C205/53
摘要： A method of synthesizing a chiral compound having a quaternary carbon atom bearing diastereotopic groups from (a) a nitroolefin and (b) an α-substituted β-dicarbonyl or an equivalent compound having an acidic C—H moiety compound is disclosed. A subsequent intramolecular reaction between one of the substituents comprising the stereogenic carbon atom and one of the diastereotopic groups comprising the quaternary carbon atom creates a new compound having two contiguous stereogenic centers, one of which is quaternary, with control over the relative stereochemistry.
摘要翻译：公开了一种合成具有（a）硝基烯烃和（b）具有酸性C-H部分化合物的α-取代的β-二羰基或等价化合物的具有非对映体基团的季碳原子的手性化合物的方法。包含立体碳原子的一个取代基和包含季碳原子的非对映体基团之一之间的随后的分子内反应产生具有两个连续的立体中心的新化合物，其中一个是季铵化合物，可控制相对的立体化学。

2. 发明授权

US5677446A Polyazacycloalkane compounds 失效
标题翻译：多氮杂环烷烃化合物
公开(公告)号：US5677446A
公开(公告)日：1997-10-14
申请号：US478754
申请日：1995-06-07
申请人： Lisa Schultze , Al Ray Bulls
发明人： Lisa Schultze , Al Ray Bulls
IPC分类号： C07D257/02 , C07D257/00
CPC分类号： C07D257/02
摘要： The present invention relates to tribenzylcyclen compounds of formula I ##STR1## (where R is hydrogen, or a C.sub.1-12 alkyl group optionally substituted by hydroxy, alkoxy or aryl groups or R is an amphiphilic aralkyl group comprising a N, S, O or P interrupted C.sub.2-25 alkylene chain, e.g. a polyalkylene oxide chain or R provides a bridge to a second tribenzylcyclen group, but with the proviso that R is other than benzyl; X is CHR.sub.1, or where R is hydrogen two X groups may each represent CO groups; and R.sub.1 is hydrogen, a C.sub.1-6 alkyl group optionally substituted by hydroxy, alkoxy or carboxy groups or an aralkyl group having 1 to 6 carbons in the alkyl moiety and optionally. substituted in the aryl moiety by alkyl, alkoxy, hydroxy or isothiocyanate groups). These compounds are useful in the preparation of DO3A, N-substituted-1,4,7,10-tetraazacyclododecane-N',N",N"'-triacetic acids, and the phosphonic acid analogs.
摘要翻译：本发明涉及式I的三苄基环化合物（I）（其中R是氢或任选被羟基，烷氧基或芳基取代的C 1-12烷基或R是包含N，S的两亲性芳烷基，O或P中断C2-25亚烷基链，例如聚环氧烷链或R提供与第二三苄基环系基团的桥连，但条件是R不是苄基; X是CHR1，或其中R是氢两个X基团可以各自表示CO基团;并且R 1是氢，任选被羟基，烷氧基或羧基取代的C 1-6烷基或在烷基部分中具有1至6个碳的芳烷基，并且任选地在芳基部分被烷基取代，烷氧基，羟基或异硫氰酸酯基）。这些化合物可用于制备DO3A，N-取代-1,4,7,10-四氮杂环十二烷-N'，N“，N” - 三乙酸和膦酸类似物。

3. 发明授权

US5631368A Polyazacycloalkane compounds 失效
标题翻译：多氮杂环烷烃化合物
公开(公告)号：US5631368A
公开(公告)日：1997-05-20
申请号：US478755
申请日：1995-06-07
申请人： Lisa Schultze , Alan R. Bulls
发明人： Lisa Schultze , Alan R. Bulls
IPC分类号： C07D257/02
CPC分类号： C07D257/02
摘要： The present invention relates to tribenzylcyclen compounds of formula I ##STR1## (where R is hydrogen, or a C.sub.1-12 alkyl group optionally substituted by hydroxy, alkoxy or aryl groups or R is an amphiphilic aralkyl group comprising a N, S, O or P interrupted C.sub.2-25 alkylene chain, e.g. a polyalkylene oxide chain or R provides a bridge to a second tribenzylcyclen group, but with the proviso that R is other than benzyl; X is CHR.sub.1, or where R is hydrogen two X groups may each represent CO groups; and R.sub.1 is hydrogen, a C.sub.1-6 alkyl group optionally substituted by hydroxy, alkoxy or carboxy groups or an aralkyl group having 1 to 6 carbons in the alkyl moiety and optionally substituted in the aryl moiety by alkyl, alkoxy, hydroxy or isothiocyanate groups). These compounds are useful in the preparation of DO3A, N-substituted-1,4,7,10-tetraazacyclododecane-N',N",N"'-triacetic acids, and the phosphonic acid analogs.
摘要翻译：本发明涉及式I的三苄基环化合物（I）（其中R是氢或任选被羟基，烷氧基或芳基取代的C 1-12烷基或R是包含N，S的两亲性芳烷基，O或P中断C2-25亚烷基链，例如聚环氧烷链或R提供与第二三苄基环系基团的桥连，但条件是R不是苄基; X是CHR1，或其中R是氢两个X基团可以各自表示CO基团;并且R 1是氢，任选地被羟基，烷氧基或羧基取代的C 1-6烷基或在烷基部分中具有1至6个碳的芳烷基，并且任选地在芳基部分被烷基，烷氧基，羟基或异硫氰酸酯基）。这些化合物可用于制备DO3A，N-取代-1,4,7,10-四氮杂环十二烷-N'，N“，N” - 三乙酸和膦酸类似物。

4. 发明授权

US5705637A Polyazacycloalkane compounds 失效
标题翻译：多氮杂环烷烃化合物
公开(公告)号：US5705637A
公开(公告)日：1998-01-06
申请号：US790855
申请日：1997-02-03
申请人： Lisa Schultze , Alan Ray Bulls
发明人： Lisa Schultze , Alan Ray Bulls
IPC分类号： C07D257/02 , C07D273/00
CPC分类号： C07D257/02
摘要： The present invention relates to tribenzylcyclen compounds of formula I ##STR1## (where R is hydrogen, or a C.sub.1-12 alkyl group optionally substituted by hydroxy, alkoxy or aryl groups or R is an amphiphilic aralkyl group comprising a N, S, O or P interrupted C.sub.2-25 alkylene chain, e.g. a polyalkylene oxide chain or R provides a bridge to a second tribenzylcyclen group, but with the proviso that R is other than benzyl; X is CHR.sub.1, or where R is hydrogen two X groups may each represent CO groups; and R.sub.1 is hydrogen, a C.sub.1-6 alkyl group optionally substituted by hydroxy, alkoxy or carboxy groups or an aralkyl group having 1 to 6 carbons in the alkyl moiety and optionally. substituted in the aryl moiety by alkyl, alkoxy, hydroxy or isothiocyanate groups). These compounds are useful in the preparation of DO3A, N-substituted-1,4,7,10-tetraazacyclododecane-N',N",N'"-triacetic acids, and the phosphonic acid analogs.
摘要翻译：本发明涉及式I的三苄基环化合物（I）（其中R是氢或任选被羟基，烷氧基或芳基取代的C 1-12烷基或R是包含N，S的两亲性芳烷基，O或P中断C2-25亚烷基链，例如聚环氧烷链或R提供与第二三苄基环系基团的桥连，但条件是R不是苄基; X是CHR1，或其中R是氢两个X基团可以各自表示CO基团;并且R 1是氢，任选被羟基，烷氧基或羧基取代的C 1-6烷基或在烷基部分中具有1至6个碳的芳烷基，并且任选地在芳基部分被烷基取代，烷氧基，羟基或异硫氰酸酯基）。这些化合物可用于制备DO3A，N-取代-1,4,7,10-四氮杂环十二烷-N'，N“，N” - 三乙酸和膦酸类似物。

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