CAS: 129-49-7; Methysergide Maleate Salt

📜N-(1-Hydroxybutan-2-yl)-7-Methyl-4,6,6A,7,8,9-Hexahydroindolo[4,3-Fg]Quinoline-9-Carboxamide 反应生成马来酸美西麦角
参考文献:1-Methyl Ergotamines And Ergocornines
标题:1-Methyl Ergotamines And Ergocornines
摘要:该发明涉及公式(i)的n1-取代的麦角酸衍生物;其中r1是甲氧基,羟基烷基氨基,氨基,单或双烷基氨基或1-吡咯烷基,或天然水不溶性麦角生物碱的三肽基团,R2是甲基,乙基,烯丙基或苄基,\sg是<;Form:0811964/iv(b)/2>;"烷基"表示含有2或3个碳原子的烷基基团.该发明还涉及通过在液氨中用碱金属酰胺处理r2为氢的公式(i)中相应的化合物,并将所得的碱金属盐与z为卤素原子的化合物r2Z反应来制备这些衍生物.最好在-30oc和-60oc之间使用甲基或乙基碘进行反应.实例描述了麦角碱,麦角胺,麦角胺,二氢麦角胺,二氢麦角甲酸,二氢麦角晶,二氢麦角酮,麦角酸和异麦角酸酰胺,麦角酸乙酰胺,二乙酰胺和吡咯烷基酰胺的1-甲基衍生物,二氢麦角晶的1-乙基衍生物,以及二氢麦角晶,二氢麦角酮和二氢麦角甲酸的1-烯丙基和1-苄基衍生物的制备.还描述了1-甲基-麦角酸二乙酰胺和吡咯烷基酰胺的酒石酸盐.

专利信息

专利号:US-4331688-A
优先权日:1978-02-23
标题 :Therapeutic method for inhibiting gastric secretion by administration of 15-deoxy-16-hydroxy prostaglandins
发明人：KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G
权利人:MILES LAB
摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.

专利号:US-4132738-A
优先权日:1978-02-23
标 题:Preparation of 15-deoxy-16-hydroxyprostaglandins
发明人：KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G
权利人:MILES LAB
摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## SUCH THAT A BICYCLOALKYL OR BICYCLOALKENYL COMPOUND IS FORMED, WHEREIN M AND N ARE INTEGERS HAVING A VALUE FROM 0 TO 3, P IS AN INTEGER HAVING A VALUE FROM 0 TO 4 AND Q IS AN INTEGER HAVING A VALUE OF FROM 1 TO 4 AND WHEREIN THE DOUBLE BOND OF SUCH BICYCLOALKENYL IS IN THE M, N, P, OR Q BRIDGE; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n Pge 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.

专利号:US-4415592-A
优先权日:1978-02-23
标 题 :15-Deoxy-16-hydroxy prostaglandins for producing bronchodilation
发明人：KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G
权利人:MILES LAB
摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 , R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.

专利号:US-4275224-A
优先权日:1978-02-23
标题:15-Deoxy-16-hydroxy prostaglandins
发明人：KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G
权利人:MILES LAB
摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 , R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.