- Practical Synthesis of a Stable Precursor for Positron Emission Tomography Imaging Agent 18F-GTP1
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18F-GTP1 is a deuterated small molecule positron emission tomography (PET) imaging agent used to visualize tau tangles in Alzheimer's disease patients. The first-generation synthesis of 18F-GTP1's nonradiolabeled alkyl tosylate precursor was plagued by low-yielding steps, inefficient chromatographic purifications, and variable product quality. Due to these limitations, a more robust second-generation route was developed and successfully executed on kilogram scale. A reduction with LiAlD4 incorporated geminal deuterium atoms, while an efficient amidation reaction accessed the key acrylamide coupling partner. Moreover, the tricyclic imidazo[1,2-a]pyrimidine core was assembled via a novel, convergent, and highly selective phosphoramidate-directed annulation. The improved synthesis eliminated all chromatography en route to a high-yielding and reproducible acid-promoted tosylation as the final step.
- Clagg, Kyle,Gosselin, Francis,Lim, Ngiap-Kie,Nack, William A.,O'Shea, Paul D.,Sirois, Lauren E.,White, Nicholas A.,Zhang, Haiming
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supporting information
p. 1690 - 1699
(2020/11/25)
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- With anti-platelet aggregation activity of the piperidinyl substituted 5- hydroxy color acid derivatives
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The invention relates to the field of pharmaceutical chemistry, particularly piperidyl substituted 5-hydroxytryptophane derivatives (I) with anti-platelet aggregation activity, and a preparation method and pharmaceutical application thereof, wherein R1, R2 and n are defined in the specification. The pharmacodynamical test proves that the piperidyl substituted 5-hydroxytryptophane derivatives have favorable anti-platelet aggregation activity.
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Paragraph 0099; 0100
(2017/02/09)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Benzothiazole derivatives with activity as adenosine receptor ligands
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The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
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- Enantio- and diastereoselective synthesis of all four possible stereoisomers of 2-(phenylhydroxymethyl)quinuclidine
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An enantio- and diastereoselective synthesis of all four possible stereoisomers of 2-(phenylhydroxymethyl)quinuclidine is reported. Key steps involve the use of the Sharpless dihydroxylation protocol to induce asymmetry, and stereodivergent cyclisations of the resulting diol to form the quinuclidine ring.
- Lygo, Barry,Crosby, John,Lowdon, Terence R.,Wainwright, Philip G.
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p. 2343 - 2346
(2007/10/03)
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- Phenoxy- and phenoxyalkyl-piperidines as antiviral agents
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Compounds of the formula STR1 wherein R1 is selected from STR2 Y is a bond or lower alkylene; R2 and R3 are independently hydrogen, lower-alkyl or halogen; R4 is STR3 R5 is hydrogen, lower-alkyl or halogen; R6 is hydrogen, lower-alkyl or halogen; R7 is hydrogen or lower-alkyl; R8 is hydrogen, lower-alkyl, or trifluoromethyl; R9 is lower-alkyl; R10 is lower-alkyl, trifluoromethyl or difluoromethyl; or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents.
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