首页> 外国专利> Condensation Reduction Methods in a single container to prepare substituted allylic alcohols, processes to obtain a quinolone Derivative of 4 - and for the separation of isomeric alcohols and other compounds

Condensation Reduction Methods in a single container to prepare substituted allylic alcohols, processes to obtain a quinolone Derivative of 4 - and for the separation of isomeric alcohols and other compounds

机译:单个容器中的缩合还原方法,用于制备取代的烯丙醇,获得4-喹诺酮衍生物的工艺,以及分离异构醇和其他化合物的方法

摘要

Condensation Reduction methods are provided in a single container to prepare substituted Allyl alcohols as well as highly Selective extraction methods to separate isomeric alcohols produced in processes of condensation reduction in a single container to prepare for and Example, a quinolone.Claim 1: a method to prepare one or more compounds of formula (1), where R1 and R2 are independently selected from h, aryl, alquiloc1 alqueniloc2 - 10, - 10 and - 10 or alquiniloc3, R1, R2, and the C Atom which can be joined together cicloalquiloc3 - 10 or heterociclilo; and R3 is Alquiloc1 alqueniloc2 h, - 10, - 10, - 10 alquiniloc3, halogen, aryl, heteroaryl or heterociclilo,Said method comprises (a) REACT in the presence of one or more bases, one or more compounds of formula R1R2 (= OR) where R1 and R2 are independently selected from aryl, alquiloc1 h, - 10, - 10 and - 10 alqueniloc2 alquiniloc3 or R1, R2 and the C Atom to which Unite together can form CIC Loalquiloc3 - 10 or heterociclilo, with a compound of formula (2) where R3 is selected from h,Alquiloc1 alqueniloc2 - 10 - 10, 10, alquiniloc3, halogen, aryl, heteroaryl, and heterociclilo, R5, R6 and R7 is independently selected from - 10 alquiloc1 and aryl; and (b) one or more additional reducing agents in the reaction of the step (a).Claim 1: a method to separate isomeric alcohols of formula (1) in a Watery mixture where R1 and R2 are different groups selected from h, alquiloc1 alqueniloc2 - 10, - 10 and - 10 or alquiniloc3, R1, R2, and the C Atom to bind together a group can be Asymmetric. Cicloalquiloc3 held between - 10 and heterociclilo replaced optionally substituted; R3 is H,Alquiloc1 - 10 not replaced, halogen, aryl, or heterociclilo, Said method comprises (a) contacting an aqueous mixture of isomeric alcohols with an appropriate volume of a non polar Solvent; and (b) Separating non polar Solvent from the aqueous layer.Claim: a method for Separating isomers of formula (3) in a solution of n-butanol where R1, R2 and the C Atom which bind together form (4); R3 is not alquiloc1 - 10 h, halogen substituted aryl, or heterociclilo; and N is 0 - 4Said method comprises (a) contacting an aqueous mixture of isomer of formula (3) with an appropriate volume of a mixture of HCl and IPA; (b) heating the resulting solution to a temperature between about 85 degrees Celsius and approximately 118u00b0C; and (c) add IPA in the resulting Solution.
机译:在单个容器中提供缩合还原方法以制备取代的烯丙醇,并在单个容器中提供高选择性萃取方法以分离在缩合还原过程中产生的异构醇以制备喹诺酮和实施例。权利要求1:一种用于制备喹诺酮的方法。制备一种或多种式(1)的化合物,其中R 1和R 2分别选自h,芳基,alquilocl alqueniloc2-10,-10和-10或alquiniloc3,R1,R2和C原子,它们可以连接在一起cicloalquiloc3 -10或异西曲洛;且R3为Alquilocl,alqueniloc2,-10,-10,-10 alquiniloc3,卤素,芳基,杂芳基或杂环基,所述方法包括(a)在一种或多种碱,一种或多种式R1R2的化合物(= OR),其中R1和R2独立选自芳基,alquiloc1h,-10,-10和10 alqueniloc2 alquiniloc3或R1,R2和C原子,它们可以联合形成CIC Loalquiloc3-10或杂环,与以下化合物式(2)其中R 3选自h,Alquiloc1 alqueniloc2-10-10、10,alquiniloc3,卤素,芳基,杂芳基和杂环基,R 5,R 6和R 7独立地选自-10 Alquiloc1和芳基;权利要求1:一种在水混合物中分离式(1)的异构醇的方法,其中R 1和R 2是选自h,alquiloc1的不同基团alqueniloc2-10,-10和-10或alquiniloc3,R1,R2和C Atom结合在一起的基团可以是不对称的。保持在-10之间的Cicloalquiloc3和被取代的杂环取代; R3是未被取代的H,Alquilocl-10,卤素,芳基或杂环基。所述方法包括:(a)使异构醇的含水混合物与适当体积的非极性溶剂接触; 1。一种在正丁醇溶液中分离式(3)异构体的方法,其中R 1,R 2和C Atom结合在一起形成(4);和(b)从水层中分离非极性溶剂。 R3不是alquiloc1-10h,卤素取代的芳基或杂环基;所述方法包括:(a)使式(3)的异构体的水性混合物与适当体积的HCl和IPA的混合物接触;和(b)将所得溶液加热至约85摄氏度至约118℃之间的温度; (c)在结果解决方案中添加IPA。

著录项

  • 公开/公告号AR063204A1

    专利类型

  • 公开/公告日2009-01-14

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号AR2007P102981

  • 发明设计人

    申请日2007-07-04

  • 分类号C07D209/48;C07D211/70;C07D401/04;C07D401/06;C07D401/14;C07C29/10;C07C29/86;

  • 国家 AR

  • 入库时间 2022-08-21 19:28:43

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