摘要:
In a method suitable for industrial application, an optically active N-aryl-β-amino acid compound is produced by the reaction of an aromatic amine and an optically active sulfonylated β-hydroxycarboxylic acid compound. The latter can be easily derived from a β-keto carboxylic acid compound.
摘要翻译:光学活性N-芳基-β-氨基酸化合物(III)的制备涉及光学活性磺酰化的β-羟基羧酸化合物和芳族胺的反应。 制备式YC * H(NH-X)-CH 2 -C(O)-Z(III)的光学活性N-芳基-β-氨基酸化合物包括使式YC的光学活性磺酰化β-羟基羧酸化合物 * H(OSO 2 R 1)-CH 2 -C(O)-Z(I)和式X-NH 2(II)的芳族胺。 Y:任选取代的甲基或芳基; Z:氨基,烷氧基或芳氧基(全部被取代)或OH; R11-10C烷基,6-15C芳基或7-20C芳烷基(全部被取代); C *:具有R或S构型的光学活性C; 和X:6-15C芳基或3-15C杂芳族(均可任意取代)。
摘要:
Novel 2-methylpropionic acid derivatives represented by general formula (I) and pharmacologically acceptable salts thereof which have an excellent beta 3 adrenaline receptor stimulating effect and are useful as preventives or remedies for obesity, hyperglycemia, diseases caused by accelerated intestinal motion, frequent urination, urinary incontinence, depression, cholelithiasis or diseases caused by accelerated biliary motion. In said Formula (I) R represents hydrogen, lower alkyl or aralkyl; R represents hydrogen, lower alkyl or halogeno; A represents oxygen or imino; the carbon atom to which (R) is attached stands for one with the R-configuration; and the carbon atom to which (S) is attached stands for one with the S-configuration.
摘要:
A process for preparing 2,3-dihydroazepine compounds of general formula (1) or salts thereof inexpensively and simply, characterized by reacting a compound of general formula (2) or a salt thereof with a compound of general formula (3) or a salt thereof to form a compound of general formula (4) or a salt thereof and subjecting the obtained compound or salt to esterification and ring-closing reaction.
摘要:
An α-iminoester derivative capable of being stably present under ordinary conditions; and a method of synthesizing various α-aminoester derivatives from the α-iminoester derivative in high yield. The derivative is a polymer-immobilized α-iminoester represented by the following general formula (1) (wherein R1 represents an alkyl chain having 1 or more carbon atoms and R2 represents hydrogen, halogeno, or optionally substituted alkyl, aryl, or alkoxy).
wherein R 1 is hydrogen or -(CH 2 ) m COOR 2 ; R 2 is hydrogen, (R 6 ) 2 N(CH 2 ) 2 -, R 6 COOCH 2 - or -CH 2 CON(CH 2 CH 2 0H) 2 ; R 3 is hydrogen, nitro, hydroxy, amino, CH 3 (CH 2 ) n S(O) 0-2 -, CH 3 (CH 2 ) n -,CH 3 (CH 2 ) n O- ,R 5 COO-, RsOOC- ,R 5 HNCOO-, RsNHCO-, RsCONH-, RsNHCONH-, [CH 3 (CH 2 ) n]2 NCO- , CH 3 (CH 2 ) n CHOHCH 2 0-, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R 8 OOC(CH 2 ) t -O, (R 6 0) 2 PO(CH 2 )pO- , (HO) (R 6 0)PO(CH 2 )pO- , R 6 [O(CH 2 ) 2 ] q O- , R 7 (CH 2 )pO-, or -O(CH 2 ) p -pyridinium + (OH - ); R 4 is CH 3 (CH 2 ) n - , CH 3 (CH 2 ) n O- , CF 3 SO 2 NH-, RsCOO-, RsOOC- ,R 5 HNCOO-, RsNHCO-, RsCONH-RsNHCONH-, [CH 3 (CH 2 ) n]2 NCO-, CH 3 (CH 2 ) n CHOHCH 2 0-, carboxy, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R 8 OOC(CH 2 ) t O-, R 6 [O(CH 2 ) 2 ] q O- , or R 7 (CH 2 )pO-; R 5 is CH 3 (CH 2 ) n -, 1-adamantyl or diphenylmethyl; R 6 is lower alkyl; R 7 is 1- or 2 -naphthyloxy, 1-, 2- or 3-pyridinyloxy, 2,3- or 3,4-dihydroxyphenyl, 6,7-dihydroxy-2-naphthyl, phenyl, phenoxy or substituted phenyl or phenoxy, wherein the substituent is selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, nitro, amino, halo, R 6 S(O) 0-2 -, carboxy, carboxy-lower alkyl or phenyl; R 8 is hydrogen or lower alkyl; n is an integer from 0 to 17; m is an integer from 1 to 3; t is an integer from 1 to 10; p is an integer from 2 to 18, and q is an integer from 1 to 6; and when R 2 is hydrogen, a pharmaceutically acceptable salt thereof with a base, are potent inhibitors of phospholipases A 2 (PLA 2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.
摘要:
Beansprucht werden Verbindungen der allgemeinen Formel II in der R¹einen Aminosäurerest oder den Rest eines Oligopeptids darstellt, in dem Aminogruppen gegebenenfalls durch Schutzgruppen substituiert sind, R², R³die gleich oder verschieden sind, Wasserstoff, eine Niederalkyl-, Niederalkoxy- Carboxy-, Niederalkoxycarbonyloder eine gegebenenfalls durch Niederalkyl substituierte Carboxamidogruppe bedeuten oder falls R² und R³ benachbart sind, eine -CH=CH-CH=CH- Gruppe darstellen, Z ein durchkonjugiertes positiv geladenes, bicyclisches heterocyclisches System und X ein Anion einer organischen oder anorganischen Säure bedeuten. Diese Verbindungen eignen sich besonders als chromogene Substrate zur Bestimmung der Aktivität von Peptidbindungen spaltenden Enzymen.
摘要:
The present disclosure relates to a compound of general formula (I):
wherein R1 and R4 are independently selected from H and COOH, R2 and R3 are independently selected from H and (CH 2 ) m COOH, in which m = 1, 2 or 3, and n is equal to 2 or 3. The present disclosure also relates to a chelate compound, which is a complex of the compound of formula (I) with a metal ion selected from the group consisting of Fe, Cu, Mg, Ca, Mn and Zn. The invention regards also the use of the compounds of formula (I) and/or their chelate complex for treating and/or preventing nutritional disorders of plants, in particular for treating and/or preventing iron chlorosis of plants.
摘要:
Phenylketone carboxylate compounds of Formula I, wherein n=2-6; R=C(0); -OC(O)- or -CH(OH)-; A is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when B is Ft B is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when A is Ft or A and B form a 5-7 membered cycloalkyl substituted with COOFt W=0, S or NFt Y=0,S,NH or CH2; m=0-2; p=1-7; have been prepared. These compounds and their pharmaceutically acceptable salts have beneficial therapeutic effects to prevent or treat a condition related to (l) blood disorders, (ii) inflammation related diseases, (iii) renal disorders and/or renal disorders complications, or (iv) fibrosis-related organ dysfunction.
摘要翻译:式I的苯甲酮羧酸酯化合物,其中n = 2-6; R = C(0); -OC(O) - 或-CH(OH) - ; 当B是Ft B是(CH 2)m COOH,W(CH 2)m COOH或YCH(COOH)((CH 2)p CH 3)时,A是(CH 2)m COOH,W(CH 2)m COOH或YCH(COOH) 当A为Ft或A和B形成被COOFt W = 0取代的5-7元环烷基时,S或NFt Y = 0,S,NH或CH 2; M = 0-2; P = 1-7; 已经准备好了 这些化合物及其药学上可接受的盐具有有益的治疗效果以预防或治疗与(1)血液病症有关的病症,(ii)炎症相关疾病,(iii)肾脏疾病和/或肾脏疾病并发症,或(iv)纤维化 - 相关器官功能障碍。