Zobrazeno 1 - 10
of 37
pro vyhledávání: '"David G. Melillo"'
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 52:514-517
A neurokinin (NK-1) receptor antagonist, [14C]Aprepitant, was synthesized using two labeled olefination reagents: [14C]dimethyltitanocene 1 and [14C]methyl (methyltrimethylsilyl)titanocene 7. Both reagents can be readily prepared from [14C]methyllith
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 50:629-633
Autor:
Dennis C. Dean, Dan Yao, Cheng-yi Chen, Charles S. Elmore, Michael A. Wallace, Jonathan Z. Ho, David G. Melillo, Matthew P. Braun
Publikováno v:
Helvetica Chimica Acta. 88:1040-1047
A simple, high-yielding synthesis of dibutyl[14C]formamide ([14C]DBF; 1) from 14CO2 was developed (Scheme 1): reaction of LiBEt3H and 14CO2 followed by aqueous workup gave H14CO2H in high yield. Conversion of the [14C]formic acid to 1 was effected by
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 48:275-283
A new synthetic methodology that captures electrophilic 35S8 with aryl Grignard reagents or lithiates provides entry to a wide variety of [35S]aryl sulfonyl chlorides upon oxidation and chlorination. Copyright © 2005 John Wiley & Sons, Ltd.
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 48:203-208
A method for scavenging excess amines in sulfur-35-labeled radioligand preparations using fluorous scavengers has been developed in an effort to simplify the purification. This fluorous scavenging has been shown to be effective at removing excess ami
Autor:
Herbert J. Jenkins, David G. Melillo, Dennis C. Dean, Anson Chang, Michael A. Wallace, Matthew P. Braun, Allen N. Jones, Xiujuan Jia, Louis S. Crocker, Rosemary Marques, David J. Schenk, Dan Yao
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 47:399-406
High-intensity ultrasonic treatment of MeOH/H2O, IPA/H2O, EtOH or H2O suspensions of C-14 labeled and unlabeled pharmaceuticals successfully reduced the average particle diameter from a range of 8–260 to 4–15 µm as determined by optical microsco
Autor:
Matthew P. Braun, Dennis C. Dean, Jonathan Z. Ho, Ying‐Duo Gao, Raju Subramanian, David G. Melillo
Publikováno v:
Helvetica Chimica Acta. 87:674-681
In support of a research program aimed at discovering orally bioavailable thrombin inhibitors, 13C- labeled 3-aminopyrazinone acetamide thrombin inhibitors have been prepared to aid in the structural elucidation of key metabolites during preclinical
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 47:115-125
Radiolabeled tracers were required for the development of a series of VLA-4 antagonists. A method to synthesize [U-14C]3,5-dichlorobenzenesulfonyl chloride was developed. From this key intermediate, various tracers were prepared in high yield. Copyri
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 46:993-1000
In support of a program to develop a new gonadotropin releasing hormone (GnRH) receptor antagonist, two 14C labelled candidate tracers, 14C-1 and 14C-2, were synthesized for utilization in metabolism studies. A slight modification of the Medicinal Ch
Autor:
Dennis C. Dean, Herb Jenkins, Yong Zhang, Carter Gibson, Allen N. Jones, David G. Melillo, Charles S. Elmore
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 45:29-36
Stable label analogues of methotrexate (MTX) and 7-hydroxymethotrexate (7-OH-MTX) were required for use as internal standards for LC/MS quantitation. A minimum incorporation of stable isotopes to produce a mass increase of 3 in the non-glutamate deri