DuPont Pharmaceuticals Company

The present route to (terminal alkynes reported by a group from the Chemical Process Department at the DuPont Pharmaceutical Company.2 This alcohol serves as a convenient starting material for the preparation of 1-acyloxy 4-mesylates 10 (eq 1). 

The DuPont Pharmaceuticals Company, Department of Chemical Physical Sciences, Experimental Station, P.O. Box 80500, Wilmington, DE, USA 19880-0500... 

RJ. Chorvat etal, US Patent 6,326,368 (December 4, 2001) Assignee DuPont Pharmaceuticals Company... 

This work was completed during the period that our group was part of the DuPont Pharmaceutical Company and its precursor, the DuPont-Merck Pharmaceutical Company. 

The established fipcos face competition not only from one another but also from start-up pharmaceutical and biopharmaceutical companies, which number about 1300 in the United States. Competition surfaces from other quarters, too. Companies like DuPont and Monsanto, which manufactured chemicals in bulk, recently entered the fi ay, respectively forming the DuPont Pharmaceutical Company and Monsanto Life Sciences. The opportunities to... 

Rodgers, J.D. Cocuzza, A.J.l,3-Benzodiazepin-2-ones and l,3-benzoxazepin-2-ones useful as HIV reverse transcriptase inhibitors (DuPont Pharmaceuticals Company, USA). WO 2000000479, 2000. 

DPC 961 (134, Scheme 2.21) has shown activity against wild-type HIV-1 and various non-nucleoside reverse transcriptase inhibitor-resistant HIV strains, and with greater potency than the structurally related efavirenz (Sustiva Bristol-Myers Squibb), an approved drug for HIV treat-ment. ° To facilitate the development of DPC 961, researchers at DuPont Pharmaceuticals Company (Wilmington, DE) developed an asymmetric conjugate addition strategy to introduce the trifluoromethyl amine stereocenter. As depicted in Scheme 2.21, treatment of the known aniline 128 ° with two equivalents of (R)-(-l-)-a-methylbenzyl isocyanate 129 afforded the hemiami-nal 130, which was subsequently converted into the 2(3//)-quinazolinone 131 by reaction with thionyl chloride and triethylamine. Reaction of the quinazolinone 131 with excess cyclopropylacetylene magnesium chloride 132 provided the dihydroquinazolinone 133 in 86% yield and 92% diastereomeric excess. Conversion of the dihydroquinazolinone 133 into DPC 961 134 involved treatment with tri-fluoroacetic acid or warm formic acid. Overall, this process provided 16 kg of DPC 961 134 in >55% overall yield from aniline 128. 

Some optimization of the original Medidnal route was reported from the DuPont Merck Pharmaceutical Company Radesca, LA., Lo, Y.S., Moore,... 

Over 100 pharmaceutical companies in the world have been applying these DuPont s air-stable coupling catalysts for the drug discovery and processes since 2001. 

Christopher T. Riley Experimental Station, DuPont Merck Pharmaceutical Company, P.O. Box 80400, Wilmington, DE 19880-0400, USA... 

Susan A. Lerke DuPont Merck Pharmaceutical Company,... 

Business case studies expanding on the areas covered in the survey, and written by sustainability leaders in major companies with chemical operations, including DuPont, Shell, BASF, GlaxoSmithKline as one major pharmaceutical company, and 3M as a major customer of chemicals. 

Benzenedicarboxamide compounds, including flubendiamide, were found through original research at NNC. However, notably, anthranilic diamides, structurally very different from benzenedicarboxamides, were discovered by DuPont [20] to have the same mode of action [21] and a couple of companies are following with patent applications Nissan Chemical [41] and Takeda Pharmaceutical Company [42] have applied for patents of the related compounds of benzenedicarboxamides, and Ishihara Sangyo Kaisha [43] has applied for patent of the related compounds of anthranilic diamides. The market entry of insecticides from this new generation could intensify competition with conventional insecticides in the future. 

Four compounds DPC-961 (128), DPC-961 (129), DPC-083 (130), and DPC-082 (131) were developed by DuPont Pharmaceuticals as non-nucleoside reverse transcriptase inhibitors. A1 the compounds have reached Phase I clinical trials DPC-083 (130) was further progressed into Phase II trials by Bristol-Myers Squibb after the company had acquired DuPont Pharmaceuticals however, the development was stopped in 2003 due to poor pharmacokinetics [135], The compounds are close analogues of Efavirenz (133) - a non-nucleoside reverse transcriptase inhibitor approved by FDA in 1998 [5], All the compounds 128-131 showed similar to Efavirenz activity towards wild-type virus in vitro however, they were more effective towards singlemutation variants and showed lower plasma serum protein binding [136,137]. 

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