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    • 4. 发明公开
    • 4,5-디히드로옥사졸-2-일벤젠 유도체의 제조방법
    • 制备4,5-二羟基-2-甲基苯并噻唑衍生物的方法
    • KR1020130075163A
    • 2013-07-05
    • KR1020110143415
    • 2011-12-27
    • 주식회사 팜한농한국화학연구원
    • 류재욱고영관김종근서지수구동완김경성최인영홍미숙김태준안희근김시용
    • C07D413/14C07D413/12C07D401/14A01N43/76
    • PURPOSE: A method for preparing 4,5-dihydrooxazol-2-ylbenzene derivatives is provided to have a relatively mild reaction condition, to easily handle a reagent, and to synthesize the 4,5-dihydrooxazol-2-ylbenzene derivatives with high yield. CONSTITUTION: A method for preparing 4,5-dihydrooxazole-2-ylbenzene compound of chemical formula 1 or a salt thereof comprises the step of cyclizing a hydroxyalkyl benzamide of chemical formula 2 under the presence of (diethylamino)sulfur trifluoride (DAST) or para-toluene sulfonate (TsOH). The cyclization is performed under the presence of a base selected from the group consisting of tray (C_1-C_6) alkyl amine, alkali metal or hydroxide of the alkali earth metal, hydroxide, and C_1-C_6 alkoxide. The base is selected from the group consisting of trimethyl amine, triethyl amine, diethyl isopropyl amine, lithium hydroxide, sodium hydroxide, calcium hydroxide, sodium hydroxide, potassium hydroxide, sodium methoxide, and potassium methoxide.
    • 目的:提供一种制备4,5-二氢恶唑-2-基苯衍生物的方法以具有相对温和的反应条件,容易处理试剂,并以高产率合成4,5-二氢恶唑-2-基苯衍生物。 构成:用于制备化学式1的4,5-二氢恶唑-2-基苯化合物或其盐的方法包括在(二乙基氨基)三氟化硫(DAST)或对位基团的存在下使化学式2的羟基烷基苯甲酰胺环化的步骤 - 甲苯磺酸盐(TsOH)。 环化是在碱土金属的碱土金属,碱金属或氢氧化物的塔板(C_1-C_6)烷基胺,碱金属或氢氧化物,C_1-C_6烷氧基化物的碱存在下进行的。 碱选自三甲胺,三乙胺,二乙基异丙胺,氢氧化锂,氢氧化钠,氢氧化钙,氢氧化钠,氢氧化钾,甲醇钠和甲醇钾组成的组。
    • 10. 发明授权
    • N-아릴알킬 파라아미노에톡시페닐아세트아미드 유도체와 그의 제조방법
    • 新型苯乙酰胺衍生物及其制备方法
    • KR1019940011149B1
    • 1994-11-24
    • KR1019910019641
    • 1991-11-06
    • 한국화학연구원
    • 박노상하덕찬최중권김현숙홍미숙이광숙
    • C07C235/20
    • The N-arylalkyl para-aminoethoxyphenyl acetamide deriv. of formula (I) and its pharmaceuticall acceptable salt is prepd. by (a) reacting a cpd. of formula (II) with a sodium azide (NaN3) to obtain a cpd. of formula (III), and (b) reducing the cpd. (III) in the presence of a carbonaceous palladium catalyst, or reacting the cpd. (III) with a triphenyl phosphine in a tetrahydrofuran solvent in the presence of water. In the formulas, X is nitro, hydroxy or amino; Y is hydrogen, halogen, hydroxy, methylene dioxy or trifluoromethyl; Z is nitro or benzyloxy; n is 2-5; p is 0-5. The cpd. (I) has good analgesic and antiinflammatory activities.
    • N-芳基烷基对氨基乙氧基苯基乙酰胺衍生物。 的式(I)化合物及其药物可接受的盐是制备的。 通过(a)反应一个cpd。 (II)与叠氮化钠(NaN 3)反应,得到cpd。 的式(III),和(b)降低cpd。 (III)在碳质钯催化剂存在下反应,或使cpd反应。 (III)与三苯基膦在四氢呋喃溶剂中在水的存在下反应。 在该式中,X是硝基,羟基或氨基; Y是氢,卤素,羟基,亚甲基二氧基或三氟甲基; Z是硝基或苄氧基; n为2-5; p为0-5。 cpd。 (I)具有良好的止痛和抗炎活性。