38473-89-1Relevant articles and documents
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
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Page/Page column 93; 317, (2020/11/23)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is -NHSO2- or -SO2NH-; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one ormore substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl,Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl andhaloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl,SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionallysubstituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno- oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
FLUORINE RADIOLABELLING PROCESS
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Page/Page column 91, (2012/02/01)
The invention relates to a process for producing a process for producing an 18F-labelled compound, the process comprising treating a compound of formula (I): wherein EDG is an electron-donating group selected from -OH, -OR4, -NHR5 and -NR55R5; R1, R2, X1 and X2 are as defined herein; and R3 is selected from H, X3 and X4, wherein X3 is a monodentate cleavable surrogate group, and X4 is a bidentate cleavable surrogate group which is bonded (a) to said X or X and (b) to the ring carbon atom para to EDG; with [18F]fluoride in the presence of an oxidant, thereby producing, when R3 in the compound of formula (I) is H, an 18F-labelled compound of formula (II), wherein EDG is as defined above and R1, R2, X1 and X2 are as defined herein; or thereby producing, when R3 in the compound of formula (I) is said monodentate cleavable surrogate group X4, a compound of formula (Ilc), wherein EDG' is O, NR5, -NR55R5 or [OR4]+, and wherein R4, R5, R55, R1, R2, X1, X2 and X3 are as defined herein; or thereby producing, when R3 in the compound of formula (I) is said bidentate cleavable surrogate group X4, a compound of formula (IIc) or a compound of formula (IId), wherein EDG' is O, NR5, -NR55R5 or [OR4]+, and wherein R4, R5, R55, R1, R2, X1, X2 and X4 are as defined herein.
The Synthesis and Structure of 3,4-Di-t-butylbenzoic Acid
Hambley, Trevor W.,Sternhell, Sever,Tansey, Charles W.
, p. 807 - 814 (2007/10/02)
3,4-Di-t-butylbenzoic acid (1) was synthesized by a seven-step sequence from 4-t-butylbenzoic acid, and its structure was determined by X-ray diffraction and refined to a residual of 0.065 for 1403 independent observed reflections.The crystals are triclinic, P1, a 6.080(1), b 8.777(1), c 13.912(3) Angstroem, α 80.76(2), β 80.84(2), γ 75.62(2)deg.It is the only example of a simple ortho-di-t-butylbenzene whose structure has been determined.The benzene ring experiences some out-of-plane distortion but, in general, strain is relieved by in-plane bond stretching and angular distortions.
