Patent classifications
C07C65/21
PROCESS FOR THE PREPARATION OF ROXADUSTAT AND ITS INTERMEDIATES
The present invention provides the process for the preparation of Roxadustat and its intermediates. Another aspect of the present invention provides a process for preparation of ethyl-5-(2-butoxycarbonyl)-4-phenoxyphenyl) oxazole-4-carboxylate of the formula (X) and its use in the preparation of Roxadustat. Another aspect of the present invention provides a process for the preparation of ethyl-4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate of the formula (XIII) and its use in the preparation of Roxadustat.
BRANCHED FLUORINE-CONTAINING COMPOUND
A novel branched fluorine-containing compound represented by formula (1):
(RfY.sub.n1LX-A).sub.n2(1)
wherein L represents a predetermined carbon-containing linker moiety; Rf, in each occurrence, is the same or different and represents fluoroalkyl optionally having at least one ether bond; Y, in each occurrence, is the same or different and represents a predetermined divalent linking group or a bond; R.sup.Y, in each occurrence, is the same or different and represents hydrogen or an organic group; L represents an (n1+n2)-valent carbon-containing linker moiety having at least one carbon atom; n1 represents a number greater than or equal to 1; n2 represents a number greater than or equal to 1; n1+n2 is a number from 3 to 6; X, in each occurrence, is the same or different and represents a divalent linking group or a bond; A, in each occurrence, is the same or different and represents ArSO.sub.3M or the like; M, in each occurrence, is the same or different and represents hydrogen, NR.sub.4, or a metal salt; and R represents hydrogen or a C.sub.1-4 organic group.
BRANCHED FLUORINE-CONTAINING COMPOUND
A novel branched fluorine-containing compound represented by formula (1):
(RfY.sub.n1LX-A).sub.n2(1)
wherein L represents a predetermined carbon-containing linker moiety; Rf, in each occurrence, is the same or different and represents fluoroalkyl optionally having at least one ether bond; Y, in each occurrence, is the same or different and represents a predetermined divalent linking group or a bond; R.sup.Y, in each occurrence, is the same or different and represents hydrogen or an organic group; L represents an (n1+n2)-valent carbon-containing linker moiety having at least one carbon atom; n1 represents a number greater than or equal to 1; n2 represents a number greater than or equal to 1; n1+n2 is a number from 3 to 6; X, in each occurrence, is the same or different and represents a divalent linking group or a bond; A, in each occurrence, is the same or different and represents ArSO.sub.3M or the like; M, in each occurrence, is the same or different and represents hydrogen, NR.sub.4, or a metal salt; and R represents hydrogen or a C.sub.1-4 organic group.
BENZENE FUSED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): is a single or double bond; n is an integer of 0 or 1; A is CH.sub.2, CH(OH), or C(O); G is C or N; X is CH.sub.2, O, or C(O); Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, NR.sub.y1R.sub.y2, OR.sub.y1, R.sub.y1C(O)R.sub.y3, C(O)R.sub.y1, C(O)OR.sub.y2, C(O)OR.sub.y2Ry3, NR.sub.y1C(O)R.sub.y2, NR.sub.y1C(O)NR.sub.y2R.sub.y3, NR.sub.y1C(O)OR.sub.y2R.sub.y3, NR.sub.y1C(O)R.sub.y2OR.sub.y3, C(O)NR.sub.y1(R.sub.y2R.sub.y3), C(O)NR.sub.y1(R.sub.y2OR.sub.y1), OR.sub.y2R.sub.y3, and OR.sub.y2OR.sub.y3, wherein each of R.sub.y1 and R.sub.y2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and R.sub.y3 is aryl optionally substituted with at least one halogen; Z is NR.sub.z1R.sub.z2, NR.sub.z1R.sub.z3, OR.sub.z1, OR.sub.z1R.sub.z3, C(O)R.sub.z1R.sub.z3, C(O)OR.sub.z1R.sub.z3, NR.sub.z1C(O)R.sub.z2R.sub.z3, NR.sub.z1C(O)OR.sub.z2R.sub.z3, C(O)NR.sub.z1R.sub.z3, or OR.sub.z2OR.sub.z3, wherein each of R.sub.z1 and R.sub.z2 is independently selected from a group consisting of H, oxygen, alkyl and aryl, and R.sub.z3 is aryl optionally substituted with at least one substituent independently selected from a group consisting of halogen, OH, R.sub.zaCOOR.sub.zb, OR.sub.zaCOOR.sub.zb, R.sub.zaSO.sub.2R.sub.zb, R.sub.zaSO.sub.2NR.sub.zbR.sub.zcR.sub.zd, R.sub.zaC(O)R.sub.zbR.sub.zc, R.sub.zaC(O)NR.sub.zbR.sub.zcR.sub.zd, RZ.sub.aC(O)NR.sub.zbSO.sub.2R.sub.zc, wherein Rza is nil or alkyl, R.sub.zb is H or alkyl, each of R.sub.zb and R.sub.zc is independently selected from a group consisting of H, OH, alkyl, aryl, alkoxyl, or NR.sub.zbR.sub.zc is a nitrogen-containing heterocyclic alkyl ring, R.sub.zd is nil or a sulfonyl alkyl group.
##STR00001##
BENZENE FUSED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): is a single or double bond; n is an integer of 0 or 1; A is CH.sub.2, CH(OH), or C(O); G is C or N; X is CH.sub.2, O, or C(O); Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, NR.sub.y1R.sub.y2, OR.sub.y1, R.sub.y1C(O)R.sub.y3, C(O)R.sub.y1, C(O)OR.sub.y2, C(O)OR.sub.y2Ry3, NR.sub.y1C(O)R.sub.y2, NR.sub.y1C(O)NR.sub.y2R.sub.y3, NR.sub.y1C(O)OR.sub.y2R.sub.y3, NR.sub.y1C(O)R.sub.y2OR.sub.y3, C(O)NR.sub.y1(R.sub.y2R.sub.y3), C(O)NR.sub.y1(R.sub.y2OR.sub.y1), OR.sub.y2R.sub.y3, and OR.sub.y2OR.sub.y3, wherein each of R.sub.y1 and R.sub.y2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and R.sub.y3 is aryl optionally substituted with at least one halogen; Z is NR.sub.z1R.sub.z2, NR.sub.z1R.sub.z3, OR.sub.z1, OR.sub.z1R.sub.z3, C(O)R.sub.z1R.sub.z3, C(O)OR.sub.z1R.sub.z3, NR.sub.z1C(O)R.sub.z2R.sub.z3, NR.sub.z1C(O)OR.sub.z2R.sub.z3, C(O)NR.sub.z1R.sub.z3, or OR.sub.z2OR.sub.z3, wherein each of R.sub.z1 and R.sub.z2 is independently selected from a group consisting of H, oxygen, alkyl and aryl, and R.sub.z3 is aryl optionally substituted with at least one substituent independently selected from a group consisting of halogen, OH, R.sub.zaCOOR.sub.zb, OR.sub.zaCOOR.sub.zb, R.sub.zaSO.sub.2R.sub.zb, R.sub.zaSO.sub.2NR.sub.zbR.sub.zcR.sub.zd, R.sub.zaC(O)R.sub.zbR.sub.zc, R.sub.zaC(O)NR.sub.zbR.sub.zcR.sub.zd, RZ.sub.aC(O)NR.sub.zbSO.sub.2R.sub.zc, wherein Rza is nil or alkyl, R.sub.zb is H or alkyl, each of R.sub.zb and R.sub.zc is independently selected from a group consisting of H, OH, alkyl, aryl, alkoxyl, or NR.sub.zbR.sub.zc is a nitrogen-containing heterocyclic alkyl ring, R.sub.zd is nil or a sulfonyl alkyl group.
##STR00001##
APPLICATION OF SYRINGIC ACID IN PROMOTING NITRIFICATION INHIBITION ACTIVITY OF DECANEDIOL
An application of syringic acid in promoting the inhibition effect of decanediol on the nitrosification activity of nitrosomonas is provided. By inhibiting the activity of a nitrosomonas, the combined use of syringic acid and 1,9-decanediol can more efficiently inhibit a nitrification process in soil and at the plant rhizosphere, increase the nitrogen use efficiency, and reduce leaching of nitrate nitrogen, thereby reducing the loss of nitrogen and discharge of the greenhouse gas nitrous oxide in a denitrification process. The addition of syringic acid in the present invention can reduce the concentration at which 1,9-decanediol functions under the equivalent condition of nitrification inhibition activity, and thus save the relative input cost.
3,6-DICHLOROSALICYLIC ACID COMPOUNDS AND RELATED SYNTHETIC PROCESSES
The present disclosure relates, in general, to 5-halo-3,6-dichlorosalicylic acid compounds, 5-halo-3,6-dichlorosalicyaldehyde compounds, processes for preparing 5-halo-3,6-dichlorosalicylic acid compounds, processes for preparing 5-halo-3,6-dichlorosalicyaldehyde compounds, processes for preparing 3,6-dichlorosalicylic acid compounds, and processes that employ such compounds as intermediates in the preparation of the herbicide dicamba.
3,6-DICHLOROSALICYLIC ACID COMPOUNDS AND RELATED SYNTHETIC PROCESSES
The present disclosure relates, in general, to 5-halo-3,6-dichlorosalicylic acid compounds, 5-halo-3,6-dichlorosalicyaldehyde compounds, processes for preparing 5-halo-3,6-dichlorosalicylic acid compounds, processes for preparing 5-halo-3,6-dichlorosalicyaldehyde compounds, processes for preparing 3,6-dichlorosalicylic acid compounds, and processes that employ such compounds as intermediates in the preparation of the herbicide dicamba.
RESIST COMPOSITION, METHOD OF FORMING RESIST PATTERN, AND COMPOUND
A resist composition including a base material component (A) whose solubility in a developing solution is changed due to the action of an acid, and a compound (D0) formed of an anion moiety and a cation moiety which is represented by Formula (d0), in which the cation moiety of the compound (D0) has a Log P value of less than 7.7. In the formula, M.sup.m+ represents an m-valent organic cation, R.sup.d0 represents a substituent, p represents an integer of 0 to 3, q represents an integer of 0 to 3, n represents an integer of 2 or greater, and a relationship of n+p(q2)+5 is satisfied.
##STR00001##
ACTIVE ESTER COMPOUND
An active ester compound that can form a cured product having excellent dielectric properties and copper foil adhesion properties is provided, a curable composition including the active ester compound is provided, and a cured product of the curable composition is provided. Also provided are a semiconductor encapsulating material, a printed wiring board, and a build-up film formed by using the curable composition. Specifically, an active ester compound is provided which includes a fluorinated hydrocarbon structural moiety and a plurality of aromatic ester structural moieties in the structure of the molecule and includes an aryloxycarbonyl structure or an arylcarbonyloxy structure at an end of the molecule, a curable composition including the active ester compound, and a cured product of the curable composition, and also provided are a semiconductor encapsulation material, a printed wiring board, and a build-up film formed by using the curable composition.