cas 747413-21-4, 1-METHYL-4-[4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)PHENYL]PIPERAZINE | Articles data ｜lookchem

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747413-21-4

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Thiazolidine derivatives or salts thereof as an active ingredient an inhibitor Pim
PROBLEM TO BE SOLVED: To provide compounds which have excellent Pim inhibitory action and are useful as pharmaceuticals.SOLUTION: A compound is a thiazolidine derivative represented by the general formula (1) in the figure, or a salt thereof. (In the formula, X represents O or S; Rrepresents a hydrogen atom or a Calkyl group; Z, Z, Z, Z, Zand Zeach independently represent CH or N; Y represents an optionally substituted, divalent Caromatic hydrocarbon group or the like; Am represents a disubstituted amino group, or an optionally substituted, nitrogen-containing saturated heterocyclic group; and Rand Reach independently represent a hydrogen atom, a halogen atom, an alkyl group or the like.)
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Paragraph 0651; 0652

(2018/10/19)

Palladium-mediated conversion of para-aminoarylboronic esters into para-aminoaryl-11C-methanes
Cross-couplings are an alternative to conventional 11C- methylations which are generally employed in PET tracer synthesis. Therefore, we set out to develop a general procedure for the synthesis of para- 11CH3 labeled aromatic amines from the corresponding para-aminoarylboronic esters in the presence of free amines. Aryl boronic esters containing primary, secondary, and tertiary amines were successfully converted into corresponding labeled methyl derivatives in sufficient radiochemical yield to apply this method for tracer development. This procedure was applied to the labeling of CIMBI-712, a promising candidate for the in vivo imaging of the 5-HT7 receptor in the CNS.
Andersen, Valdemar L.,Herth, Matthias M.,Lehel, Szabolcs,Knudsen, Gitte M.,Kristensen, Jesper L.
supporting information
p. 213 - 216
(2013/02/22)

PEPTIDASE INHIBITORS
Novel compounds of the formula (I) wherein R1, R2, D, A, B and X have the meanings defined herein, pharmaceutical compositions comprising them as active ingredient, as well as their use in medicine, in particular as peptidase inhibitors, more specifically
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(2012/10/18)

QUINOXALINE DERIVATIVES AS INHIBITORS OF THE TYROSINE KINASE ACTIVITY OF JANUS KINASES
The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R6 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases
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Page/Page column 49-50

(2009/01/24)

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Chemical Properties

Melting Point: 112-114°C
Boiling Point: 419.2 °C at 760 mmHg
Flash Point:207.3 °C
Density: 1.07 g/cm³
Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C
Vapor Pressure: 3.09E-07mmHg at 25°C
Refractive Index: 1.542
PKA: 7.78±0.42(Predicted)
PSA: 24.94000
LogP: 1.74050

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