Novartis/Ciba-Geigy

USAN Valsartan Trade name Diovan Novartis/Ciba-Geigy Launched 1997 M.W. 425.52... 

The synthesis of valsartan (2) by Novartis/Ciba-Geigy chemists is highlighted in Scheme 9.5. Biphenylbenzyl bromide 18 is converted to biphenyl acetate 19 in the presence of sodium acetate in acetic acid. Hydrolysis of 19 followed by Swern oxidation delivered the biphenyl aldehyde 20, which underwent reductive amination with (L)-valine methyl ester (21) to give biphenyl amino acid 22. Acylation of 22 with penta-noyl chloride (23) afforded biphenyl nitrile 24, which is reacted with tributyltin azide to form the tetrazole followed by ester hydrolysis and acidihcation to provide valsartan (2). [See Biihlmayer et al. (1994, 1995).]... 

Scheme 9.5. The Novartis/Ciba-Geigy synthesis of valsartan (2).

Novartis (Ciba Geigy) has developed ferrocenyldiphosphines, 4, for the asymmetric hydrogenation of sterically hindered /V-aryl imines, specifically for the industrial manufacture of Meto-lachlor (52), a pesticide sold since March 1997 as the enantiomerically enriched form under the trade name DUAL MAGNUM and, more recently, Dual Gol (see Chapters 15 and 31).73 76 The synthesis of 52 involves the asymmetric reduction by a catalyst formed in situ from [Ir(COD)Cl]2 and 4h to give 53 and subsequently 52 in 80% ee (Scheme 12.15).74... 

Novartis (Ciba Geigy) has reported the synthesis of Benazepril (163) (Scheme 12.63), an angiotensin-converting enzyme inhibitor, via an intermediate prepared by cinchona-modified Pt asymmetric hydrogenation (10-200-kg scale, >98%, 79-82% ee).5 The low optical purities can be tolerated because enantio-enrichment is relatively easy in the latter stages of the synthesis.22... 

Novartis (Ciba Geigy) has implemented a cinchona-modified Pt/Al203 catalyst in the asymmetric hydrogenation of a-keto esters for the industrial preparation of Benzaprin. 

Trasidrex (Novartis)-comb. USA Navidrix (Ciba-Geigy) ... 

D Desferal (Ciba) I Desferal (Ciba-Geigy) USA Desferal (Novartis as... 

F Desferal (Ciba-Geigy) J Desferal (Novartis-Takeda) mesylate)... 

Oradol (Novartis-Takeda) USA Bradosol Bromide (Ciba-Geigy) wfm... 

Lopresor (Novartis 1978) Seloken (Astra 1978) Selozide (Astra)-comb. Lopresor (Ciba-Geigy) Seloken (Fujisawa 1983) Lopressor (Novartis 1978)... 

The. selective hydrogenation of a nitro group in the presence of other reactive functionalities is a frequently encountered problem in fine chemicals manufacture. Ciba-Geigy (Novartis). scientists developed, in collaboration with a catalyst manufacturer, a new Pt/Pb on CaCO. catalyst that allows the chemoselective hydrogenation of an aromatic nitro group in the presence of C=C, C=0, C=N as well as Cl or Br substituents in selectivities > 95% (even C C groups react very slowly) (Bader et al., 1996). Eqn. (3) shows an example (Bader eJ a/., 1996). 

A fascinating example of enantioselective catalysis for agrochemicals is the production of a well-known herbicide of Novartis (formerly Ciba Geigy), metolachlor (Trade name Dual... 

Solvias (spin-off from Ciba-Geigy/Novartis) Proprietary chiral ligands, process R D. Several production processes, many pilot- and bench-scale applications [141]. 

By 1995, Ciba-Geigy (now Novartis) and NeuroSpheres had entered into a collaborative research agreement for the treatment of CNS disorders with stem cells however, no development has been reported on the project by Ciba-Geigy since then [200025]. 

Ritalin has been hailed by many parents and teachers as a miracle pill once described by its makers (Novartis, formerly Ciba-Geigy Pharmaceuticals) as a mild central nervous system stimulant and by the New York Times as a mild stimulant that is roughly [equivalent to] a jolt of strong coffee. 24 These statements belie the fact that Ritalin has been known, since it was first marketed in the mid-1950s, to be a highly addictive drug subject to widespread abuse. 

As the DEA was taking the usual steps to prepare its preliminary response, in which it planned to deny CHADD s petition, the Merrow Report (a team of journalists) produced a television documentary on the ADHD-Ritalin epidemic. When it aired on PBS in October 1995, the documentary revealed a connection between Ritalin s manufacturer—then Ciba-Geigy, now Novartis—and CHADD. Ciba-Geigy had contributed nearly 900,000 to CHADD over five years, a fact... 

Ciba-Geigy/Novartis - United States (1-10,12)b Shell/DuPont - United States (1.12)... 

---