Method for producing alkenylthiophenols and their esters
    31.
    发明授权
    Method for producing alkenylthiophenols and their esters 失效
    制备烯基硫酚及其酯的方法

    公开(公告)号:US4794205A

    公开(公告)日:1988-12-27

    申请号:US940675

    申请日:1986-12-10

    CPC classification number: C07C323/00 C07C327/00 C07C45/46 C07C45/54

    Abstract: A method is provided for preparing alkenylthiophenols, e.g., para-vinylthiophenol, or their esters, e.g., para-vinylthiophenol acetate by reacting a hydroxy aromatic ketone, e.g., 4-hydroxyacetophenone (4-HAP) with an N,N-di(organo)thiocarbamoyl halide, e.g., N,N-dimethylthiocarbamoyl chloride (DMTC) to form an O-(acylaryl) N,N-di(organo)thiocarbamate, e.g., O-(4'-acetophenyl) N,N-dimethylthiocarbamate, and pyrolytically rearranging the latter compound to form an S-(acylaryl) N,N-di(organo)thiocarbamate, e.g., S-(4-4- -acetophenyl) N,N-dimethylthiocarbamate. In one procedure, the latter compound is directly reduced to form an S-(1-hydroxyalkylaryl) N,N-di(organo) thiocarbamate, e.g., S-[4'-(1-hydroxyethyl)phenyl] N,N-dimethylthiocarbamate, which is either hydrolyzed to form a (1-hydroxyalkyl) thiophenol, e.g., 4'-(1-hydroxyethyl) thiophenol, which optionally after acylation of its thiol group, is dehydrated to form the alkenylthiophenol wherein the double bond is at the ring-bonded carbon atom, e.g., para-vinylthiophenol, or the S-(1-hydroxyalkylaryl) N,N-di(organo) thiocarbamate is dehydrated to form an S-(alkenylaryl) N,N-di(organo) thiocarbamate, e.g., S-(4-vinylphenyl) N,N-dimethylthiocarbamate which is hydrolyzed to form the alkenylthiophenol. In an alternative procedure, the S-(acylaryl) N,N-di(organo)thiocarbamate is hydrolyzed and the resulting thiol acylated with an acylating agent, e.g., acetyl chloride, to produce an acylthiophenol ester, e.g., 4-acetothiophenol acetate, which is then reduced and hydrolyzed to produce the (1-hydroxyalkyl) thiophenol. The latter compound is then dehydrated to produce the alkenylthiophenol, or acylated and dehydrated to produce alkenylthiophenol thioester, as described in the first procedure.

    Abstract translation: 提供了通过使羟基芳族酮(例如4-羟基苯乙酮(4-HAP))与N,N-二(有机酮)反应制备烯基硫酚,例如对乙烯基苯硫酚或其酯,例如对乙烯基苯硫酚乙酸酯的方法 )硫代氨基甲酰卤,例如N,N-二甲基硫代氨基甲酰氯(DMTC)以形成O-(酰基芳基)N,N-二(有机)硫代氨基甲酸酯,例如O-(4'-乙酰苯基)N,N-二甲基硫代氨基甲酸酯和 热解地重新排列后一种化合物以形成S-(酰基芳基)N,N-二(有机))硫代氨基甲酸酯,例如S-(4- 4-乙基苯基)N,N-二甲基硫代氨基甲酸酯。 在一个方法中,将后一种化合物直接还原形成S-(1-羟基烷基芳基)N,N-二(有机基)硫代氨基甲酸酯,例如S- [4' - (1-羟乙基)苯基] N,N-二甲基硫代氨基甲酸酯 ,其被水解形成(1-羟基烷基)苯硫酚,例如任选在其硫醇基团酰化之后的4' - (1-羟乙基)苯硫酚脱水形成链烯基苯硫酚,其中双键位于环上 例如对 - 乙烯基苯硫酚或S-(1-羟基烷基芳基)N,N-二(有机))硫代氨基甲酸酯脱水形成S-(烯基芳基)N,N-二(有机))硫代氨基甲酸酯,例如 ,S-(4-乙烯基苯基)N,N-二甲基硫代氨基甲酸酯,其被水解形成烯基苯硫酚。 在另一种方法中,S-(酰基芳基)N,N-二(有机))硫代氨基甲酸酯被水解,所得到的硫醇用酰化剂(例如乙酰氯)酰化,得到酰基苯硫酚酯,例如4-乙酰苯硫酚乙酸酯, 然后将其还原并水解以产生(1-羟基烷基)苯硫酚。 然后将后一种化合物脱水以产生烯基苯硫酚,或者如第一步所述将其酰化和脱水以制备链烯硫基苯硫酚硫酯。

    Antihistamine and anti-nausea pharmaceutical compositions for topical application
    32.
    发明申请
    Antihistamine and anti-nausea pharmaceutical compositions for topical application 审中-公开
    用于局部应用的抗组胺药和抗恶心药物组合物

    公开(公告)号:US20080255103A1

    公开(公告)日:2008-10-16

    申请号:US11786715

    申请日:2007-04-12

    CPC classification number: A61K9/0014 A61K47/34 A61K47/36 A61K47/44

    Abstract: A topical pharmaceutical preparation suitable for use as an antihistamine or anti-nausea drug comprises an emu oil gel base and a therapeutic amount of promethazine.HCl. The preparation may further comprise an antioxidant. The preparation is preferably packaged as a single unit dose. A method for preparing the topical pharmaceutical preparation comprises the steps of combining a clear gel with an emu oil mixture and adding a therapeutic amount of promethazine.HCl solution.

    Abstract translation: 适合用作抗组胺药或抗恶心药物的局部药物制剂包括em u油凝胶基质和治疗量的异丙嗪。 该制剂还可以包含抗氧化剂。 该制剂优选包装为单一单位剂量。 制备局部药物制剂的方法包括将澄清凝胶与em油混合物混合并加入治疗量的异丙嗪.HCl溶液的步骤。

    Process for preparing coumarin sulfonates
    33.
    发明授权
    Process for preparing coumarin sulfonates 失效
    香豆素磺酸盐的制备方法

    公开(公告)号:US5773591A

    公开(公告)日:1998-06-30

    申请号:US813106

    申请日:1997-03-07

    CPC classification number: C07D311/56

    Abstract: A novel process for preparing sulfonic acid esters and amides of benzo-heterocyclic diazo diketo compounds, such as substituted diazo-4-oxo-3,4-dihydrocoumarins, which are useful synthetic intermediates in a wide variety of applications including photoresists, opto-electronics, agricultural, and pharmaceutical applications is disclosed and claimed. The process comprises the steps of (a) subjecting a substituted benzo-heterocyclic .beta.-keto-enol compound to suitable diazo transfer conditions in the presence of a diazo transfer agent; (b) subjecting the so formed diazo diketo compound to suitable halosulfonation conditions in the presence of a halosulfonation agent; and (c) subjecting the so formed halosulfonyl aromatic compound to suitable substitution reaction in the presence of an alcohol or an amine to form the corresponding sulfonic acid ester or amide of benzo-heterocyclic diazo diketo compound. The compounds formed from the process of the present invention exhibit very high photosensitivity in the deep ultraviolet (DUV) region (ca. 250 nm), and therefore, are useful as photoactive compounds in DUV photoresist formulations.

    Abstract translation: 一种用于制备苯并杂环重氮二酮化合物的磺酸酯和酰胺的新方法,例如取代的重氮-4-氧代-3,4-二氢香豆素,其在各种应用中是有用的合成中间体,包括光致抗蚀剂,光电子 ,农业和药物应用被公开和要求保护。 该方法包括以下步骤:(a)在重氮转移剂存在下使取代的苯并杂环的β-酮 - 烯醇化合物进行合适的重氮转移条件; (b)在卤代磺化剂的存在下使如此形成的重氮二酮化合物进行适当的卤代磺化条件; 和(c)使这样形成的卤代磺酰基芳族化合物在醇或胺的存在下进行适当的取代反应,形成相应的苯并杂环重氮二酮化合物的磺酸酯或酰胺。 由本发明方法形成的化合物在深紫外(DUV)区域(约250nm)中表现出非常高的光敏性,因此可用作DUV光致抗蚀剂制剂中的光活性化合物。

    Use of 4-substituted 2-butanones to prepare nabumetone
    35.
    发明授权
    Use of 4-substituted 2-butanones to prepare nabumetone 失效
    使用4-取代的2-丁酮制备萘丁酮

    公开(公告)号:US5600009A

    公开(公告)日:1997-02-04

    申请号:US629656

    申请日:1996-04-09

    CPC classification number: C07C49/255 C07C45/62 C07C45/68 C07C45/71

    Abstract: The palladium-catalyzed coupling of aryl and vinyl halides with vinylic compounds is disclosed. A preferred embodiment relating to the palladium catalyzed coupling of 4-substituted and 6-substituted-2-methoxynaphthalene to form nabumetone is also disclosed. The beauty of this novel reaction is that methylvinylketone, normally employed by the art directly as-is for the preparation of nabumetone, is formed in situ. We have discovered a mechanism to take advantage of the in situ formation of methylvinylketone, thus avoiding the use of expensive, toxic, and unstable methyl vinyl ketone feed. This reaction may be employed for a variety of pharmaceutically active and non-pharmaceutical compounds.

    Abstract translation: 公开了芳基和乙烯基卤化物与乙烯基化合物的钯催化偶联。 还公开了涉及4-取代的和6-取代-2-甲氧基萘形成萘丁酮的钯催化偶联的优选实施方案。 这种新型反应的优点是本领域直接用于制备萘丁酮的甲基乙烯基酮原位形成。 我们已经发现了利用甲基乙烯酮原位形成的机制,从而避免使用昂贵的,有毒的和不稳定的甲基乙烯基酮进料。 该反应可用于多种药物活性和非药物化合物。

    Diamond film structures and methods related to same
    36.
    发明授权
    Diamond film structures and methods related to same 失效
    金刚石薄膜结构和方法相关

    公开(公告)号:US5488350A

    公开(公告)日:1996-01-30

    申请号:US178784

    申请日:1994-01-07

    CPC classification number: H01C7/048 H01L23/3732 H01L2924/0002

    Abstract: Novel structures are provided including laminated layers of the diamond film in different patterns for conducting, generating and/or absorbing thermal energy. In particular, a thermal sensor/heater is shown including a doped electrically conductive diamond film layer encapsulated by layers of undoped electrically insulative layers on a silicon wafer. Also, a GaAs/Si on diamond laminate structure is provided in which the diamond film acts as a substrate and a heat sink. Notably, the diamond film structures are characterized by their high thermal conductivity, high chemical resistance, and high hardness/wear resistance due to the properties of the diamond films.

    Abstract translation: 提供新颖的结构,包括用于导电,产生和/或吸收热能的不同图案的金刚石膜的层压层。 具体地,示出了热传感器/加热器,其包括在硅晶片上由未掺杂的电绝缘层的层封装的掺杂导电金刚石膜层。 此外,提供了一种金刚石层叠结构的GaAs / Si,其中金刚石膜用作衬底和散热器。 值得注意的是,由于金刚石膜的性质,金刚石膜结构的特征在于其高导热性,高耐化学性和高硬度/耐磨性。

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