Large-Scale Practical Synthesis of Boc-Protected 4-Fluoro-l-Proline

2020 ◽  
Vol 24 (9) ◽  
pp. 1609-1613
Author(s):  
Yasinalli Tamboli ◽  
Bharat Kashid ◽  
Ram Prasad Yadav ◽  
Mohammad Rafeeq ◽  
Arvind Y Merwade
2011 ◽  
Vol 8 (62) ◽  
pp. 1281-1297 ◽  
Author(s):  
Lulu Qian ◽  
Erik Winfree

The prospects of programming molecular systems to perform complex autonomous tasks have motivated research into the design of synthetic biochemical circuits. Of particular interest to us are cell-free nucleic acid systems that exploit non-covalent hybridization and strand displacement reactions to create cascades that implement digital and analogue circuits. To date, circuits involving at most tens of gates have been demonstrated experimentally. Here, we propose a simple DNA gate architecture that appears suitable for practical synthesis of large-scale circuits involving possibly thousands of gates.


Synthesis ◽  
2017 ◽  
Vol 50 (05) ◽  
pp. 1015-1019 ◽  
Author(s):  
Kazutaka Matoba ◽  
Yoshiaki Nishibayashi ◽  
Aya Eizawa ◽  
Shunsuke Nishimura ◽  
Kazuya Arashiba ◽  
...  

A synthetic method for N-heterocyclic carbene- and phosphine-based PCP-type pincer ligand is described on a large scale. Some transition-metal complexes bearing the PCP-type pincer ligand are prepared and characterized by X-ray crystal structure analysis.


2009 ◽  
Vol 2009 (7) ◽  
pp. 420-422 ◽  
Author(s):  
Sheng Yin Zhao ◽  
Hong Yu Liang ◽  
Zhi Yu Shao ◽  
Rui Chen

A practical synthesis of 1-cyano-4,5-dimethoxybenzocyclobutene, the key intermediate of Ivabradine, was developed in four or five steps using two different routes. 2-Bromo-4,5-dimethoxyhydrocinnamonitrile was produced via the condensation of 2-bromo-4,5-dimethoxybenzaldehyde with acetonitrile or cyanoacetic acid and reduction by NaBH4. Cyclisation gave 1-cyano-4,5-dimethoxybenzocyclobutene. Overall yields of the routes A and B were 30% and 37% respectively. Route B is a short and simple route, permitting the synthesis of 1-cyano-4,5-dimethoxybenzocyclobutene on a large scale.


2021 ◽  
Vol 17 ◽  
pp. 2906-2914
Author(s):  
Yuki Yamamoto ◽  
Akihiro Tabuchi ◽  
Kazumi Hosono ◽  
Takanori Ochi ◽  
Kento Yamazaki ◽  
...  

A simple and efficient method for α-brominating lactones that affords α-bromolactones under mild conditions using tetraalkylammonium hydroxide (R4N+OH−) as a base was developed. Lactones are ring-opened with Br2 and a substoichiometric amount of PBr3, leading to good yields of the corresponding α-bromocarboxylic acids. Subsequent intramolecular cyclization over 1 h using a two-phase system (H2O/CHCl3) containing R4N+OH− afforded α-bromo lactones in good yields. This method can be applied at the 10 mmol scale using simple operations. α-Bromo-δ-valerolactone, which is extremely reactive and difficult to isolate, could be isolated and stored in a freezer for about one week using the developed method. Optimizing the solvent for environmentally friendly large-scale syntheses revealed that methyl ethyl ketone (MEK) was as effective. In addition, in situ-generated α-bromo-δ-valerolactone was directly converted into a sulfur-substituted functional lactone without difficulty by reacting it with a sulfur nucleophile in one pot without isolation. This new bromination system is expected to facilitate the industrial use of α-bromolactones as important intermediates.


1994 ◽  
Vol 4 (13) ◽  
pp. 1613-1618 ◽  
Author(s):  
Takehiro Fukami ◽  
Toshio Nagase ◽  
Toshiaki Mase ◽  
Akira Naya ◽  
Kagari Fujita ◽  
...  

2001 ◽  
Vol 66 (3) ◽  
pp. 1057-1060 ◽  
Author(s):  
Michael J. Totleben ◽  
J. Siva Prasad ◽  
James H. Simpson ◽  
Steven H. Chan ◽  
Dale J. Vanyo ◽  
...  

1983 ◽  
Vol 61 (3) ◽  
pp. 562-564 ◽  
Author(s):  
Chiu-Ming Wong ◽  
Hing-Yat Lam ◽  
Wasimul Haque ◽  
Ai-Qiao Mi ◽  
Gui-Shu Yang

The important intermediate 2-acetyl-5,8-dimethoxytetralin (8) in the syntheses of anthracycline antitumor drugs is easily prepared in high yield on a large scale. Conversion of 2,4-pentanedione to 3-(2,5-dimethoxybenzyl)-hex-5-en-2-one (9) was carried out in a three-step, one-pot process by C-alkylating it with 2,5-dimethoxybenzyl bromide, then allyl bromide followed by a retro-Claisen condensation. Conversion of 9 to the tetralin (8) was done first by ozonolysis to the aldehyde (10) followed by cyclization and reduction of the latter by trimethylsilane in trifluoracetic acid – acetone.


1999 ◽  
Vol 173 ◽  
pp. 243-248
Author(s):  
D. Kubáček ◽  
A. Galád ◽  
A. Pravda

AbstractUnusual short-period comet 29P/Schwassmann-Wachmann 1 inspired many observers to explain its unpredictable outbursts. In this paper large scale structures and features from the inner part of the coma in time periods around outbursts are studied. CCD images were taken at Whipple Observatory, Mt. Hopkins, in 1989 and at Astronomical Observatory, Modra, from 1995 to 1998. Photographic plates of the comet were taken at Harvard College Observatory, Oak Ridge, from 1974 to 1982. The latter were digitized at first to apply the same techniques of image processing for optimizing the visibility of features in the coma during outbursts. Outbursts and coma structures show various shapes.


1994 ◽  
Vol 144 ◽  
pp. 29-33
Author(s):  
P. Ambrož

AbstractThe large-scale coronal structures observed during the sporadically visible solar eclipses were compared with the numerically extrapolated field-line structures of coronal magnetic field. A characteristic relationship between the observed structures of coronal plasma and the magnetic field line configurations was determined. The long-term evolution of large scale coronal structures inferred from photospheric magnetic observations in the course of 11- and 22-year solar cycles is described.Some known parameters, such as the source surface radius, or coronal rotation rate are discussed and actually interpreted. A relation between the large-scale photospheric magnetic field evolution and the coronal structure rearrangement is demonstrated.


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