Process for the preparation of nitrodiaryl sulfoxides
    15.
    发明授权
    Process for the preparation of nitrodiaryl sulfoxides 失效
    制备硝基二芳基亚砜的方法

    公开(公告)号:US4831194A

    公开(公告)日:1989-05-16

    申请号:US76675

    申请日:1987-07-23

    IPC分类号: A01N41/10 A61K31/10

    摘要: The invention relates to a new process for the preparation of aminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein X is halogen, alkoxy having from 1 to 6 carbon atoms or a group --(N,R,R.sup.1), in which p1 R and R.sup.1 are hydrogen or alkyl having from 1 to 6 carbon atoms,R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or phenyl or phenylthio both optionally substituted by one or more identical or different halogen(s) and/or amino group(s),and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular are potent anthelmintics, or can be used as active ingredients in pesticidal compositions. The invention therefore relates to pharmaceutical and pesticidal compositions containing compounds of formula (I) or salts thereof as active ingredient.Compounds of formula (I), in which the substituents are as defined above, but if X stands for a group --N(R,R.sup.1) in which R and R.sup.1 both represent hydrogen, and X is in para-position related to the sulfoxide group, then R.sup.2 is other than hydrogen, halogen, alkyl having from 1 to 6 carbon atoms and alkoxy having from 1 to 6 carbon atoms, and the acid addition salts thereof, are new. These new compounds are also subject of the present invention.

    摘要翻译: 本发明涉及制备式(I)的氨基二芳基亚砜衍生物的新方法,其中X是卤素,具有1至6个碳原子的烷氧基或基团 - (N,R 1,R 2, ),其中p1 R和R1是氢或具有1至6个碳原子的烷基,R2是氢,卤素,具有1至6个碳原子的烷基,具有1至6个碳原子的烷氧基或苯基或苯硫基, 通过一个或多个相同或不同的卤素和/或氨基,及其酸加成盐。 式(I)的化合物是药学活性的,特别是有效的驱肠虫剂,或可用作杀虫组合物中的活性成分。 因此,本发明涉及含有式(I)化合物或其盐作为活性成分的药用和杀虫组合物。 式(I)的化合物,其中取代基如上所定义,但如果X代表基团-N(R,R 1),其中R和R 1都代表氢,并且X在对位上与亚砜相关 基团,则R2不是氢,卤素,具有1至6个碳原子的烷基和具有1至6个碳原子的烷氧基及其酸加成盐是新的。 这些新化合物也是本发明的主题。

    Nintrovincaminic acid derivatives having pharmaceutical utility
    17.
    发明授权
    Nintrovincaminic acid derivatives having pharmaceutical utility 失效
    具有药用效用的新一代氨基酸衍生物

    公开(公告)号:US4810709A

    公开(公告)日:1989-03-07

    申请号:US105959

    申请日:1987-10-07

    CPC分类号: C07D461/00

    摘要: The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) ##STR1## wherein R stands for a --CO--X group, wherein X means a halogen atom; orfor a --CO--OR.sup.1 group, wherein R.sup.1 means an optionally mono- or polysubstituted C.sub.1-10 aliphatic group, a C.sub.3-8 alicyclic group or an aromatic C.sub.6-14 hydrocarbyl group; orfor a --CO--NR.sup.2 R.sup.3 group, wherein R.sup.2 and R.sup.3 are the same or different and stand for a hydrogen atom or a C.sub.1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R.sup.3 may also represent an amino group when R.sup.2 stands for a hydrogen atom; orfor a cyano group,as well as their salts and pharmaceutical preparations containing these compounds. Furthermore the invention relates to a process for preparing these compounds and preparations.The racemic and optically active substances of the general formula (I) as well as their pharmaceutically acceptable acid addition and quaternary salts have valuable therapeutic properties, namely vasodilating, spasmolytic, antihypoxic and anticonvulsive effects.

    摘要翻译: 本发明涉及制备通式(I)的新型外消旋和光学活性的9-或11-硝基
    氨基嘌呤酸衍生物的新方法,其中R代表-CO-X基团,其中X表示 卤素原子; 或-CO-OR 1基团,其中R 1表示任选的单取代或多取代的C 1-10脂族基团,C 3-8脂环族基团或芳族C 6-14烃基; 或-CO-NR 2 R 3基团,其中R 2和R 3相同或不同,代表氢原子或任选地与相邻的氮原子一起形成饱和杂环的C 1-8烷基,并且任选地与一个或多个另外的氮 原子或其它杂原子,当R 2代表氢原子时,R 3也可以表示氨基; 或氰基,以及它们的含有这些化合物的盐和药物制剂。 此外,本发明涉及一种制备这些化合物和制剂的方法。 通式(I)的外消旋和光学活性物质及其药学上可接受的酸加成盐和季盐具有有价值的治疗性质,即血管舒张,解痉,抗缺氧和抗惊厥作用。

    Process for continuous drying of chemical products by
milling-fluidisation
    18.
    发明授权
    Process for continuous drying of chemical products by milling-fluidisation 失效
    通过研磨流化连续干燥化学产品的方法

    公开(公告)号:US3938259A

    公开(公告)日:1976-02-17

    申请号:US533087

    申请日:1974-12-16

    摘要: A process for the continuous drying of chemical products by milling fluidization, in which a fluidized bed of particles of an inert carrier, e.g., quartz sand having a particle diameter of 0.5-1.0 mm., is maintained and the chemical product to be dried is introduced in a wet state, e.g., wet solid or paste or suspension, into the fluidized carrier bed. The chemical product dries on the surface of the inert carrier particles and dry particles of the chemical product leave the relatively large and heavy carrier particles and are carried off in the exit gas. The carrier particles, however, are too large and heavy to leave in the exit gas and so remain in the fluidized bed. If desired, the dried product particles can be further dried, for example by additional drying gas in a cyclone chamber, after which the dried particles are separated from the gas which can be vented and/or recycled.

    摘要翻译: 通过研磨流化连续干燥化学产品的方法,其中维持惰性载体颗粒的流化床,例如粒径为0.5-1.0mm的石英砂,待干燥的化学产品为 以湿态(例如,湿固体或糊状物或悬浮液)引入流化载体床。 化学产品在惰性载体颗粒的表面上干燥,化学产品的干燥颗粒留下相对较大和重的载体颗粒,并在出口气体中被排出。 然而,载体颗粒太大而重,不能留在出口气体中,因此残留在流化床中。 如果需要,干燥的产物颗粒可以进一步干燥,例如通过旋风室中的另外的干燥气体干燥,然后将干燥的颗粒与可以排出和/或再循环的气体分离。