摘要:
Selective production of a dialkanolamine is attained by controlling the volume preceding the entrance to a catalyst bed and the temperature prevailing under respectively fixed levels subsequent to the mixture of an alkylene oxide thereby repressing a reaction occurring in the absence of a catalyst and curbing the formation of trialkanolamine. The reactant fluid is prevented from generating a channeling by disposing an exportable structure in a reactor thereby creating the state of a false shell-and-tube type reactor. The reaction is initiated with the inlet temperature set at a higher level than the prescribed level and the alkylene oxide concentration set at a lower level than the prescribed level and thereafter the inlet temperature and the alkylene oxide concentration are gradually changed toward the respectively prescribed levels.
摘要:
Phenylethanolamine compounds represented by general formula (I) and pharmacologically acceptable salts thereof which have a potent effect of stimulating β3 adrenaline receptors and a high selectivity for β3 adrenaline receptors, wherein R1 represents hydrogen or halogeno; R2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted by one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted by lower alkylaminocarbonyl optionally substituted by lower alkoxy, lower alkoxy substituted by cyclic C4-6 aminocarbonyl, lower alkoxycarbonyl, or carboxy; R3 represents hydrogen, hydroxy, lower alkoxy, or lower alkoxy substituted by one or two lower alkoxycarbonyl or carboxy groups, or R2 and R3 may be bonded to each other to thereby form methylenedioxy substituted by carboxy or lower alkoxycarbonyl; and m and n are each 0 or 1.
摘要翻译:本发明涉及由通式AIU代表phenylethanolamines化合物:(其中R1 darstellt氢或卤素; R 2 darstellt氢,羟基,低级烷氧基,低级烷氧基substituiertem被一个或两个低级烷氧基羰基或羧基,低级烷氧基substituiertem与 低级烷基氨基羰该管道可与低级烷氧基,低级烷氧基substituiertem具有4至6个碳原子的环状氨基羰基,低级烷氧基羰或羧基; R 3 darstellt氢,羟基,低级烷氧基或低级烷氧基substituiertem被一个或两个低级烷氧基羰基或羧基; R2和R3可键合到彼此,以形成具有羧基或低级烷氧羰基亚甲二氧基substituiertem;和m和n是0或1),和它们的药理学上可接受的盐,它们具有有效的β3肾上腺素能刺激作用和高的β3肾上腺素能受体 选择性,以及其生产方法及其生产中间体的方法。
摘要:
A process for the preparation of 3-amino-2-hydroxy-1-propyl ethers of general formula (4), (wherein R1 is alkyl, or an aromatic or heterocyclic group; and R?2 and R3¿ are each hydrogen or alkyl, or alternatively they together with the nitrogen atom may form a cyclic amine), characterized by reacting an epoxy compound of general formula (1), (wherein X is halogeno or sulfonyloxy) with an alcohol in the presence of a fluorine salt and reacting the obtained product with an amine. The process enables the preparation of intermediates for the synthesis of drugs in high yields and at a high optical purity.
摘要翻译:制备通式(4)的3-氨基-2-羟基-1-丙醚的方法,(其中R 1是烷基或芳族或杂环基; R 2和R 3各自是氢或烷基 ,或者它们与氮原子一起形成环胺),其特征在于通式(1)(其中X是卤代或磺酰氧基)的环氧化合物与醇在氟盐存在下反应, 用胺得到产物。 该方法能够以高收率和高光学纯度制备用于合成药物的中间体。
摘要:
A process is provided for producing a 2-amino-1phenylethanol derivative comprising;
allowing (a) a compound shown by the general Formula (III)
or (b) a compound shown by the general Formula (IV)
wherein R 1 , R 2 , R 3 , R 4 and R 5 represent a hydrogen atom etc; Z represents a hydrogen atom or a protective group for hydroxyl group and X represents a halogen atom, to react with a compound of the Formula Y-NH 2 wherein Y represents a hydrogen atom or a group which can be left in the reaction, further, when Y is the group which can be left in the reaction, allowing Y to be left, to obtain a compound shown by the general Formula (VI)
which comprises adding an acid to the reaction products containing the compound of the general Formula (VI) to precipitate or crystallize said compound as a salt and, thereby, isolating the compound of the general Formula (VI).
摘要:
This invention relates to a novel solution phase process for the preparation of tertiary amine combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.
摘要:
This invention relates to a novel solution phase process for the preparation of tertiary amine combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.
摘要:
An (R)-2-amino-1-phenylethanol derivative shown by the general formula (Ila) wherein R 1 and R 5 represent a hydrogen atom, etc.; R 2 , R 3 and R 4 independently represent a halogen atom, etc., or a salt thereof, can readily be produced (1) by permitting a microorganism belonging to the genus Rhodosporidium, the genus Comamonas or the like to act on a mixture of corresponding (R)-form and (S)-form to asymmetrically utilize, or (2) by permitting a microorganism belonging to the genus Lodderomyces, the genus Pilimelia or the like to act on a corresponding aminoketone derivative to asymmetrically reduce. An (R,R)-1-phenyl-2-[(2-phenyl-1-alkylethyl) amino]ethanol derivative having a high optical purity can easily be obtained from the compound of the formula (Ila) or a salt thereof. Said derivative is useful as an intermediate for producing an anti-obesity agent and so on.
摘要:
A method for scavenging mercaptans in hydrocarbon fluid is disclosed. According to the method, an effective mercaptan-scavenging amount of an aqueous scavenging composition is added to the fluid. The composition comprises a quaternary ammonium hydroxide of the formula R¹R²R³R⁴NOH. R¹ and R² are, independently, alkyl groups of from one to about eighteen carbon atoms, aryl groups of from six to about eighteen carbon atoms or alkylaryl groups of from seven to about eighteen carbon atoms. R³ is an alkyl group of from two to about eighteen carbon atoms, an aryl group of from two to about eighteen carbon atoms or an alkylaryl group of from four to about eighteen carbon atoms. R² and R³ may be joined to form a heterocyclic ring including the N and optionally an oxygen atom. R⁴ is -(CH₂CH₂O)nH, wherein n is an integer from one to about eighteen, or -CHR⁵CHR⁶Y, wherein R⁵ and R⁶ are, independently, hydrogen, alkyl groups of from one to about eighteen carbon atoms, aryl groups of from six to about eighteen carbon atoms or alkylaryl groups of from seven to about eighteen carbon atoms. Y is a non-acidic group. A method of preparing certain such quaternary ammonium hydroxides is also disclosed.
摘要翻译:公开了一种在烃流体中清除硫醇的方法。 根据该方法,将有效的硫醇清除量的清除水的组合物加入到流体中。 组合物包含式R 1 R 2 R 4 NOH的季铵氢氧化物。 R 1和R 2独立地为1至约18个碳原子的烷基,6至约18个碳原子的芳基或7至约18个碳原子的烷基芳基。 R 3是具有2至约18个碳原子的烷基,2至约18个碳原子的芳基或4至约18个碳原子的烷基芳基。 R 2和R 3可以连接形成包括N和任选的氧原子的杂环。 R 4为 - (CH 2 CH 2 O)n H,其中n为1至约18的整数,或-CHR 5 CHR 6,其中R 5和R 6独立地为氢, 1至约18个碳原子的烷基,6至约18个碳原子的芳基或7至约18个碳原子的烷基芳基。 Y是非酸性基团。 还公开了制备某些这种氢氧化铵的方法。
摘要:
Verfahren zur Herstellung von tensidischen Anion-Kation-Komplexen, wobei man eine kohlenstoff- oder siliciumorganische Verbindung mit mindestens einer Epoxidgruppe mit einem quaternären Ammoniumhydrogensulfit der allgemeinen Formel
HN ⊕ (R¹)₃SO₃H ⊖ ,
wobei
R¹ innerhalb des Moleküls gleich oder verschieden ist und
(1) ein Alkyl- oder Hydroxyalkylrest mit 1 bis 18 Kohlenstoffatomen, (2) ein Phenylrest oder (3) ein Rest der Formel C n H 2n+1 CONH-(CH₂) m -, in der n eine Zahl von 7 bis 17 und m = 2 oder 3 ist, sein kann,
in Gegenwart eines polaren Lösungsmittels in solchen Mengen umsetzt, daß das Molverhältnis Epoxidgruppe : HN ⊕ (R¹)₃SO₃H ⊖ 2 : 1 beträgt.