Rearrangement Approaches to Cyclic Skeletons. IX. Stereoselective Total Synthesis of (±)-Camphorenone Based on a Ring-Contraction of Bicyclo[3.2.1]oct-6-en-2-one. Reliable One-Step Diazo Transfer Followed by a Wolff Rearrangement

1995 ◽  
Vol 68 (9) ◽  
pp. 2687-2694 ◽  
Author(s):  
Tadao Uyehara ◽  
Naohiko Takehara ◽  
Masako Ueno ◽  
Toshio Sato
Keyword(s):  
Total Synthesis ◽  
Wolff Rearrangement ◽  
Ring Contraction ◽  
One Step

Radiosynthesis of a Novel PET Fluoronicotinamide for Melanoma Tumour PET Imaging; [18F]MEL050

2011 ◽  
Vol 64 (7) ◽  
pp. 873 ◽  
Author(s):  
Ivan Greguric ◽  
Stephen Taylor ◽  
Tien Pham ◽  
Naomi Wyatt ◽  
Cathy D. Jiang ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Large Scale ◽  
Radiochemical Purity ◽  
Specific Activity ◽  
Phase 1 ◽  
Radiochemical Yield ◽  
Synthesis Time ◽  
Clinical Phase ◽  
One Step ◽  
No Carrier Added

[18F]6-Fluoro-N-[2-(diethylamino)ethyl]nicotinamide [18F]MEL050 is a novel nicotinamide-based radiotracer, designed to target random metastatic dissemination of melanoma tumours by targeting melanin. Preclinical studies suggest that [18F]MEL050 has an excellent potential to improve diagnosis and staging of melanoma. Here we report the radiochemical optimization conditions of [18F]MEL050 and its large scale automated synthesis using a GE FXFN automated radiosynthesis module for clinical, phase-1 investigation. [18F]MEL050 was prepared via a one-step synthesis using no-carrier added K[18F]F-Krytpofix® 222 (DMSO, 170°C, 5 min) followed by HPLC purification. Using 6-chloro-N-[2-(diethylamino)ethyl]nicotinamide as precursor, [18F]MEL050 was obtained in 40–46% radiochemical yield (non-decay corrected), in greater than 99.9% radiochemical purity and specific activity ranging from 240 to 325 GBq μmol–1. Total synthesis time including formulation was 40 min and [18F]MEL050 was stable (99.8%) in PBS for 6 h.

scholarly journals One‐Step Synthesis of 2,5‐Diaminoimidazoles and Total Synthesis of Methylglyoxal‐Derived Imidazolium Crosslink (MODIC)

2019 ◽  
Vol 131 (52) ◽  
pp. 19089-19093
Author(s):  
Venkata R. Sabbasani ◽  
Kung‐Pern Wang ◽  
Matthew D. Streeter ◽  
David A. Spiegel
Keyword(s):  
Total Synthesis ◽  
One Step

Total Synthesis of (−)-Pavidolide B: A Ring Contraction Strategy

2019 ◽  
Vol 84 (14) ◽  
pp. 9385-9392 ◽  
Author(s):  
Peirong Rao ◽  
Jialei Hu ◽  
Jun Xuan ◽  
Hanfeng Ding
Keyword(s):  
Total Synthesis ◽  
Ring Contraction

A Diastereoselective Total Synthesis oftrans-Trikentrin A: A Ring Contraction Approach

2008 ◽  
Vol 10 (23) ◽  
pp. 5417-5420 ◽  
Author(s):  
Luiz F. Silva ◽  
Marcus V. Craveiro
Keyword(s):  
Total Synthesis ◽  
Ring Contraction ◽  
Trikentrin A
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