专利号:EP-0310950-B1 优先权日:1983-11-18 标题 :Quinoline intermediates for the synthesis of 1H-imidazo[4,5-c]quinolines and 1H-imidazo[4,5-c]quinolin-4-amimes 摘要:Compounds of the types (I) and (II) are disclosed, wherein each R5 is independently selected from the group consisting of alkyl of one to about four carbon atoms, alkoxy of one to about four carbon atoms and halogen, and n is an integer from 0 to 2, with the proviso that if n is 2, then said R5 substituents together contain no more than 6 carbon atoms; R6 is selected from the group consisting of hydroxyalkyl of one to about six carbon atoms and cyclohexylmethyl; and R7 is selected from the group consisting of alkyl of one to about four carbon atoms and hydrogen. These compounds may be used as intermediates for the synthesis of 1H-imidazo[4,5-c]quinoline derivatives.
专利号:US-7153967-B2 优先权日:2002-07-23 标题:Preparation of 1H-imidazo [4,5-C] quinolin-4-amines via 1H-imidazo [4,5-C] quinolin-4-phthalimide intermediates 发明人:MERLI VALERIANO; MANTOVANI SILVIA; BIANCHI STEFANO 权利人:TEVA GYOGYSZERGYAR ZARTKOERUEE 摘要:The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.
专利号:US-7335772-B2 优先权日:2002-07-26 标 题:1H-imidazo [4,5-c] quinolin-4-cyano and 1H-imidazo [4,5-c] quinolin-4-carboxamide intermediates 发明人:MERLI VALERIANO; MANTOVANI SILVIA; BIANCHI STEFANO 权利人:TEVA GYOGYSZERGYAR ZARTKOERUEE 摘要:The invention relates to a process for the synthesis of 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1 H-imidazo[4,5-C]quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C]quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C]quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-carboxamide, and to the said intermediates.
专利号:US-6069149-A 优先权日:1997-01-09 标 题:Amide derivatives and intermediates for the synthesis thereof 发明人:NANBA RYOUICHI; IIZUKA TAKAO; ISHII TAKEO 权利人:TERUMO CORP 摘要:PCT No. PCT/JP98/00005 Sec. 371 Date Nov. 23, 1998 Sec. 102(e) Date Nov. 23, 1998 PCT Filed Jan. 6, 1998 PCT Pub. No. WO98/30562 PCT Pub. Date Jul. 16, 1998Novel compounds which are amide derivatives represented by general formula (I) and medicinal preparations containing the same having an eosinophilic infiltration inhibitory effect based on a potent interferon ( alpha , gamma )-inducing activity and an exellent percutaneous absorbability and being efficacious in treating allergic inflammatory diseases such as atopic dermatitis, various tumors and viral diseases. In said formula, each symbol has the following meaning: R1 and R2: each lower alkyl, etc.; X and Y: independently representing each oxygen, NR4, CR5 etc. (wherein R4 and R5 independently represent each hydrogen, an aromatic group, etc.); Z: an aromatic ring or heterocycle; R3: hydrogen, lower alkoxy, etc.; g, i and k: independently representing each an integer of from 0 to 6; h, i and l: independently representing each an integer of 0 or 1; m: an integer of from 0 to 5; and n: an integer of from 2 to 12.
专利号:CN-113461679-B 优先权日:2021-06-29 标题 :Synthesis of a Benzazepine Isatin Compound
专利号:DE-3486043-T2 优先权日:1983-11-18 标 题:INTERMEDIATE CHINOLINE PRODUCTS FOR THE SYNTHESIS OF 1H-IMIDAZO (4,5-C) QUINOLINES AND 1H-IMIDAZO (4,5-C) QUINOLIN-4-AMINES.
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003). 摘要:Lindsley, C. W.; Layton, M. E., Science of Synthesis, (2004) 17, 411.