128495-64-7Relevant academic research and scientific papers
One-pot chemoenzymatic synthesis of trolline and tetrahydroisoquinoline analogues
Zhao, Jianxiong,Lichman, Benjamin R.,Ward, John M.,Hailes, Helen C.
, p. 1323 - 1326 (2018/02/14)
Chemoenzymatic reaction cascades can provide access to chiral compounds from low-cost starting materials in one pot. Here we describe one-pot asymmetric routes to tetrahydroisoquinoline alkaloids (THIAs) using the Pictet-Spenglerase norcoclaurine synthase (NCS) followed by a cyclisation, to give alkaloids with two new heterocyclic rings. These reactions operated with a high atom economy to generate THIAs in high yields.
Synthesis and bioevaluation of [18F]4-fluoro-m- hydroxyphenethylguanidine ([18F]4F-MHPG): A novel radiotracer for quantitative PET studies of cardiac sympathetic innervation
Jang, Keun Sam,Jung, Yong-Woon,Sherman, Phillip S.,Quesada, Carole A.,Gu, Guie,Raffel, David M.
, p. 1612 - 1616 (2013/04/10)
A new cardiac sympathetic nerve imaging agent, [18F]4-fluoro-m- hydroxyphenethylguanidine ([18F]4F-MHPG), was synthesized and evaluated. The radiosynthetic intermediate [18F]4-fluoro-m-tyramine ([18F]4F-MTA) was prepared and then sequentially reacted with cyanogen bromide and NH4Br/NH4OH to afford [ 18F]4F-MHPG. Initial bioevaluations of [18F]4F-MHPG (biodistribution studies in rats and kinetic studies in the isolated rat heart) were similar to results previously reported for the carbon-11 labeled analog [11C]4F-MHPG. The neuronal uptake rate of [18F]4F-MHPG into the isolated rat heart was 0.68 ml/min/g wet and its retention time in sympathetic neurons was very long (T1/2 >13 h). A PET imaging study in a nonhuman primate with [18F]4F-MHPG provided high quality images of the heart, with heart-to-blood ratios at 80-90 min after injection of 5-to-1. These initial kinetic and imaging studies of [18F]4F-MHPG suggest that this radiotracer may allow for more accurate quantification of regional cardiac sympathetic nerve density than is currently possible with existing neuronal imaging agents.
Synthesis and Dopamine Receptor Affinities of 2-(4-fluoro-3-hydroxyphenyl)ethylamine and N-Substituted Derivatives
Claudi, Francesco,Cardellini, Mario,Cingolani, Gian Mario,Piergentili, Alessandro,Pertuzzi, Guidubaldo,Balduini, Walter
, p. 2408 - 2412 (2007/10/02)
The synthesis of 2-(4-fluoro-3-hydroxyphenyl)ethylamine (26) and of some N,N-dialkyl derivatives (27-30) starting from 4-fluoro-3-hydroxytoluene and their in vitro binding affinities for dopamine (DA) receptor are reported.The amine 26 can be regarded as
