Volume 18; Issue 12

Organic Process Research & Development

Volume 18; Issue 12

1

Improved Process for Pilot-Scale Synthesis of Danshensu ((±)-DSS) and Its Enantiomer Derivatives

Bai, Yajun, Zhang, Qunzheng, Jia, Pu, Yang, Lingjian, Sun, Yuhong, Nan, Yefei, Wang, Shixiang, Meng, Xue, Wu, Yizhen, Qin, Fanggang, Sun, Zhe, Gao, Xiaokang, Liu, Pei, Luo, Kai, Zhang, Yajun, Zhao, Xi

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 326 KB

english, 2014

2

Development of a Safe, Scalable Process for the Preparation of an Oxaisoxazolidinone

Santhosh, U., Kshirsagar, Yogesh M., Venkatesan, K., Hazra, Debasis, Kindel, Jnaneshwara, Sridharan, R., Ennis, David, Howells, Garnet E., Stefinovic, Marijan, Manjunatha, Sulur G., Nambiar, Sudhir

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 314 KB

english, 2014

3

Development of a Modeling-Based Strategy for the Safe and Effective Scale-up of Highly Energetic Hydrogenation Reactions

Mitchell, Christopher W., Strawser, Josiah D., Gottlieb, Alex, Millonig, Michael H., Hicks, Frederick A., Papageorgiou, Charles D.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 1.15 MB

english, 2014

4

A Method for Heteroaromatic Nitration Demonstrating Remarkable Thermal Stability

Beutner, Gregory L., Desai, Lopa, Fanfair, Dayne, Lobben, Paul, Anderson, Eric, Leung, Simon W., Eastgate, Martin D.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 1.11 MB

english, 2014

5

Synthesis of Akt Inhibitor Ipatasertib. Part 1. Route Scouting and Early Process Development of a Challenging Cyclopentylpyrimidine Intermediate

Lane, Jonathan W., Spencer, Keith L., Shakya, Sagar R., Kallan, Nicholas C., Stengel, Peter J., Remarchuk, Travis

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 686 KB

english, 2014

6

Development of a Practical and Scalable Synthetic Route to YM758 Monophosphate, A Novel I f Channel Inhibitor

Yoshida, Shinya, Marumo, Kiyotaka, Takeguchi, Kazuhiro, Takahashi, Takumi, Mase, Toshiyasu

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 423 KB

english, 2014

7

Palladium on Charcoal as a Catalyst for Stoichiometric Chemo- and Stereoselective Hydrosilylations and Hydrogenations with Triethylsilane

Tuokko, Sakari, Pihko, Petri M.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 613 KB

english, 2014

8

Short Synthesis of a Proline Amide Orexin Receptor Antagonist on the Pilot Plant Scale

Tortoioli, Simone, Marchal, Daniel, Kesselgruber, Martin, Pabst, Thomas, Skranc, Wolfgang, Abele, Stefan

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 522 KB

english, 2014

9

Practical Asymmetric Hydrogenation-Based Synthesis of a Class-Selective Histone Deacetylase Inhibitor

Chen, Junli, Chen, Tianqi, Hu, Qiupeng, Püntener, Kurt, Ren, Yi, She, Jin, Du, Zhengming, Scalone, Michelangelo

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 723 KB

english, 2014

10

Continuous Reductions and Reductive Aminations Using Solid NaBH 4

Gilmore, Kerry, Vukelić, Stella, McQuade, D. Tyler, Koksch, Beate, Seeberger, Peter H.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 384 KB

english, 2014

11

Using Aryl Diazonium Salts in Palladium-Catalyzed Reactions under Safer Conditions

Oger, Nicolas, d’Halluin, Martin, Le Grognec, Erwan, Felpin, François-Xavier

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 6.18 MB

english, 2014

12

Development of a Practical Process for the Opening of Macrocyclic Cyclosporin A and Amino Acid Deletion

Riss, Bernard, Grandeury, Arnaud, Gut, Thorsten, Seeger-Weibel, Manuela, Zuercher, Christian, Li, Jinjing, Gallou, Fabrice

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 888 KB

english, 2014

13

Investigation on Main Reaction and Side Reaction Mechanism in the Synthetic Process of 1-(5-Bromothiophen-2-yl)-3-(4-nitrophenyl)prop-2-en-1-one Using Raman Spectroscopy

Huang, Jiajun, Hao, Hongxun, Wang, Yongli, Bao, Ying, Ye, Wei, Xie, Chuang, Yin, Qiuxiang, Sun, Zhihong

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 454 KB

english, 2014

14

Synthesis of Akt Inhibitor Ipatasertib. Part 2. Total Synthesis and First Kilogram Scale-up

Remarchuk, Travis, St-Jean, Frederic, Carrera, Diane, Savage, Scott, Yajima, Herbert, Wong, Brian, Babu, Srinivasan, Deese, Alan, Stults, Jeffrey, Dong, Michael W., Askin, David, Lane, Jonathan W., Sp

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 1.10 MB

english, 2014

15

An Improved and Efficient Process for the Preparation of Tofacitinib Citrate

Patil, Yogesh S., Bonde, Nilesh L., Kekan, Ankush S., Sathe, Dhananjay G., Das, Arijit

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 418 KB

english, 2014

16

Effects of Diluents on the Reaction Hazards of Tributyl Phosphate with Nitric Acid

Sreekantan, Smitha Velayuthan, Mahadevan, Surianarayanan, Jala, Samuel Vara Kumar, Seshadri, Hariharan, Mandal, Asit Baran

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 4.48 MB

english, 2014

17

Diastereospecific Enolate Addition and Atom-Efficient Benzimidazole Synthesis for the Production of L/T Calcium Channel Blocker ACT-280778

Funel, Jacques-Alexis, Brodbeck, Stephan, Guggisberg, Yves, Litjens, Remy, Seidel, Thomas, Struijk, Martin, Abele, Stefan

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 1.02 MB

english, 2014

18

Practical Large-Scale Synthesis of 6-Bromo-2-naphthylmethanesulfonamide Using Semmler–Wolff Reaction

Li, Wenke, Towne, Timothy B., Liang, Guangxin, Haight, Anthony R., Barnes, David M.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 411 KB

english, 2014

19

Safe Scale-Up of Pharmaceutical Manufacturing Processes with Dimethyl Sulfoxide as the Solvent and a Reactant or a Byproduct

Wang, Zhe, Richter, Steven M., Bellettini, John R., Pu, Yu-Ming, Hill, David R.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 2.60 MB

english, 2014

20

Applications of Gage Reproducibility & Repeatability (GRR): Understanding and Quantifying the Effect of Variations from Different Sources on a Robust Process Development

Deshpande, Amol A., Ramya, Ayyalasomayajula, Vishweshwar, Vavilala, Deshpande, Girish R., Roy, Amrendra Kumar

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 1.56 MB

english, 2014

21

Some Items of Interest to Process R&D Chemists and Engineers

Zhao, Wenyi, Zhao, Dongbo, Guizzetti, Sylvain, Raghuraman, Arjun, Schwindeman, James A., Knight, John

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 844 KB

english, 2014

22

Safety Notables: Information from the Literature

Dale, David, Ironside, Michael D., Shaw, Stephen M.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 287 KB

english, 2014

23

Lab-Scale Preparation of a Novel Carbocyclic Chemokine Receptor Antagonist

Teleha, Christopher A., Branum, Shawn, Zhang, Yongzheng, Reuman, Michael E., Van Der Steen, Luc, Verbeek, Marc, Fawzy, Nagy, Leo, Gregory C., Kang, Fu-An, Cai, Chaozhong, Kolpak, Michael, Beauchamp, D

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 391 KB

english, 2014

24

Safety Special Feature Editorial

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 110 KB

english, 2014

25

Application of In Situ Raman Spectroscopy To Facilitate Use of Hydrogen Peroxide on Kilogram Scale

Cohen, Dawn, Cosbie, Andrew, Milburn, Robert R., Shaw, Stephen, Xie, Yong

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 668 KB

english, 2014

26

Lab-Scale Preparation of a Novel Cyclopenta[b]furan Chemokine Receptor Antagonist

Teleha, Christopher A., Branum, Shawn, Zhang, Yongzheng, Reuman, Michael E., Van Der Steen, Luc, Verbeek, Marc, Fawzy, Nagy, Leo, Gregory C., Winters, Michael P., Kang, Fu-An, Kolpak, Michael, Beaucha

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 509 KB

english, 2014

27

Green Chemistry Articles of Interest to the Pharmaceutical Industry

Bandichhor, Rakeshwar, Bhattacharya, Apurba, Diorazio, Louis, Dunn, Peter, Fraunhoffer, Kenneth, Gallou, Fabrice, Hayler, John, Hickey, Matthew, Hinkley, Bill, Humphreys, Luke, Kaptein, Bernard, Mathe

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 1.04 MB

english, 2014

28

Editorial: Out with the Old, In with the New. Dr. Kai Rossen Takes Over as Editor-in-Chief of Organic Process Research & Development

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 114 KB

english, 2014

29

Kiloscale Buchwald–Hartwig Amination: Optimized Coupling of Base-Sensitive 6-Bromoisoquinoline-1-carbonitrile with ( S )-3-Amino-2-methylpropan-1-ol

Sperry, Jeffrey B., Price Wiglesworth, Kristin E., Edmonds, Ian, Fiore, Phillip, Boyles, David C., Damon, David B., Dorow, Roberta L., Piatnitski Chekler, Eugene L., Langille, Jonathan, Coe, Jotham W.

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 707 KB

english, 2014

30

Development of a Scalable Synthesis of Oligomeric Piperidine- N - O -alkyl Ethers

Cote, Everett, Chafin, Laura, DiFazio, Mike, Robbins, Jim, Kotrola, Joe, Nocentini, Tiziano, Schoening, Kai-Uwe

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 711 KB

english, 2014

31

Synthesis of an α-Amylase Inhibitor: Highly Stereoselective Glycosidation and Regioselective Manipulations of Hydroxyl Groups in Carbohydrate Derivatives

Ueda, Tsuyoshi, Hayashi, Masaki, Ikeuchi, Yutaka, Nakajima, Takumi, Numagami, Eiji, Kobayashi, Satoshi

Journal:

Organic Process Research & Development

Year:

2014

Language:

english

File:

PDF, 1.32 MB

english, 2014

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