16726-41-3Relevant academic research and scientific papers
Decarboxylative hydrazination of unactivated carboxylic acids by cerium photocatalysis
Yatham, Veera Reddy,Bellotti, Peter,K?nig, Burkhard
supporting information, p. 3489 - 3492 (2019/03/26)
We report the cerium photocatalyzed radical decarboxylative hydrazination of carboxylic acids with di-tert-butylazodicarboxylate (DBAD). The operationally simple protocol provides rapid access to synthetically useful hydrazine derivatives and overcomes current scope limitations in the photoredox-catalyzed decarboxylation of carboxylic acids.
Synthesis method for pharmaceutically acceptable salt of alkylhydrazine
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Paragraph 0051; 0052, (2017/08/28)
The invention discloses a synthesis method for pharmaceutically acceptable salt of alkylhydrazine. According to the method, with hydrazine hydrate and BOC anhydride as starting raw materials, BOC hydrazine is synthesized firstly, then alkyl compounds are added in, BOC alkylhydrazine is obtained, finally BOC is removed, and the pharmaceutically acceptable salt of the corresponding alkylhydrazine is obtained in a conversion manner. According to the synthesis method, the raw materials for use are low in price and cost and easy to obtain. The synthesis method is short in synthesis route and high in yield, the obtained product is high in chemical purity, special production equipment is not needed for all reactions, and obtained intermediates and the final product do not need column chromatography and crystallization and purification.
1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones as PDE1 Inhibitors
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Paragraph 0197; 0198, (2017/10/30)
The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
PROTEIN KINASE INHIBITORS
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Paragraph 0236, (2015/07/15)
The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.
PYRAZOLO[3,4-D]PYRIMIDIN-4(5H)-ONE DERIVATIVES AS PDE9 INHIBITORS
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Page/Page column 21; 22, (2014/02/16)
A compound of the general formula (I) wherein R1 is selected from the group consisting of phenyl unsubstituted or substituted with 1 to 3 substituents selected from F, Cl, Br, I, CN, -O-C1-C3-alkyl, fluorinated -O-C1-C3-alkyl, -(CH2)mOH and 5-membered heterocyclic group with 1 or 2 heteroatoms selected from N, O and S; and 6- or 10-membered heteroaryl with 1 to 3 heteroatoms selected from O, N and S; R2 and R3 independently of each other represent H atom or straight or branched C1-C3 alkyl; R4 is selected from the group consisting of 4- to 6- membered cycloalkyl, wherein one of carbon atoms can be replaced by O atom, and which is unsubstituted or substituted with one or two halogen atoms,and straight or branched C1-C4 alkyl; Q represents a bond or C1-C3-alkylene, which can be optionally substituted by one to three C1-C3-alkyls; X is selected from the group consisting of O, NR5, and S(O)p; R5 represents H atom or C1-C3alkyl; m is 1, 2 or 3; p is 0, 1 or 2; and salts thereof, for use as a medicament, in particular for treating cognitive function disorders and neurodegenerative diseases.
PROCESS FOR MAKING BENZOXAZEPIN COMPOUNDS
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Page/Page column 9; 24, (2014/09/29)
Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula (I), having the structure: Formula (I) (GDC-0032), and intermediates useful for the preparation of (I).
Reactions of grignard reagents with nitrous oxide
Tskhovrebov, Alexander G.,Solari, Euro,Scopelliti, Rosario,Severin, Kay
supporting information, p. 2405 - 2408 (2014/06/10)
The chemical activation of nitrous oxide (N2O) can be achieved by organocalcium, organosodium, and organolithium compounds. Grignard reagents, on the other hand, are believed to be inert. We demonstrate that this generalization is not correct. Some aliphatic Grignard reagents undergo a rapid conversion when subjected to an atmosphere of N2O. Hydrazones are the main reaction products.
PROTEIN KINASE INHIBITORS
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Page/Page column 77-78, (2014/01/07)
The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.
Imidazoline derivatives as alpha-1A adrenoceptor ligands
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Page/Page column 34, (2010/02/11)
Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.
ANTIBACTERIAL AGENTS
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Page 18-19, (2010/02/07)
Compounds of formula (I) have antibacterial activity, wherein Q represents -N(OH)CH(=O) or -C(=O)NH(OH); Y represents -C(=O)-, - C(=S)-, -S(=O)-, or -SO2-; R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of formula -N(OH)CH(=O), a hydroxy, Cl-C6 alkoxy, Cl-C6 alkenyloxy, halogen, amino, Cl-C6 alkylamino, or di-( C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, C1-C3 alkyl-O-Cl-C3 alkyl, Cl-C3 alkyl-S-C1-C3 alkyl, cycloalkyl(C1-C3 alkyl)-, aryl(C1-C3 alkyl)-, heterocyclyl(C1-C3 alkyl)-, or R1R2N-C1-C3 alkyl group wherein R1 represents hydrogen or Cl-C3 alkyl and R2 represents Cl-C3 alkyl, or R1R2N- represents a cyclic amino group; R3 and R5 independently represent hydrogen or a substituted or unsubstituted C1-C6 alkyl group or R3 and R5 taken together with the carbon and nitrogen atoms to which they are respectively attached form a saturated heterocyclic ring of from 5 to 7 ring atoms, which may be fused to a second carbocyclic or heterocyclic ring, either of which rings may optionally be substituted; R4 represents hydrogen or a substituted or unsubstituted Cl-C6 alkyl, C2--C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, heterocyclyl, Cl-C3 alkyl-O-CI-C3 alkyl, C1--C3 alkyl-S-C1-C3 alkyl, C1-C3 alkyl-NH-(CI-C3 alkyl)-, cycloalkyl(C1-C3 alkyl)-, heterocyclic(C1-C3 alkyl)- or aryl(C1-C3 alkyl)- group; and A represents a primary, secondary or tertiary amino group or a group -R6, -OR6, wherein R6 is a substituted or unsubstituted Cl-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, heterocyclyl, C1-C3 alkyl-O-(C1-C3 alky)-l, C1-C3 alkyl-S-(C1-C3 alkyl)-, Cl-C3 alkyl--NH-(C1-C3 alkyl)-, cycloalkyl(C1-C3 alkyl)-, heterocyclic(C1-C3 alky)-l or aryl(C1-C3 alkyl)- group.
