Search Results - "La Cruz, Thomas"

Practical olefin hydroamination with nitroarenes by Gui, Jinghan, Pan, Chung-Mao, Jin, Ying, Qin, Tian, Lo, Julian C., Lee, Bryan J., Spergel, Steven H., Mertzman, Michael E., Pitts, William J., La Cruz, Thomas E., Schmidt, Michael A., Darvatkar, Nitin, Natarajan, Swaminathan R., Baran, Phil S.

“…The synthesis and functionalization of amines are fundamentally important in a vast range of chemical contexts. We present an amine synthesis that repurposes…”
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Multicomponent Synthesis of 1‑Aryl 1,2,4-Triazoles by Tam, Annie, Armstrong, Ian S, La Cruz, Thomas E

“…A multicomponent (single reactor) process for the synthesis of 1-aryl 1,2,4-triazoles was explored and developed. This transformation prepared the…”
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Implementation of a mathematical model for the photochemical kinetics of a solid form active pharmaceutical ingredient by La Cruz, Thomas E., Carvalho, Thiago C., Ramírez, Antonio, Tábora, José E.

“…[Display omitted] We present here the development of a photochemical model used to quantify the risk to photodegradation of a solid drug substance. A key…”
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Scalable Asymmetric Synthesis of the All Cis Triamino Cyclohexane Core of BMS-813160 by La Cruz, Thomas E, González-Bobes, Francisco, Eastgate, Martin D, Sfouggatakis, Chris, Zheng, Bin, Kopp, Nathaniel, Xiao, Yi, Fan, Yu, Galindo, Kay A, Pathirana, Charles, Galella, Michael A, Deerberg, Joerg

“…BMS-813160 is a pharmaceutical entity currently in development at Bristol Myers Squibb. Its defining structural feature is a unique chiral all cis triamino…”
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Leveraging AQbD Principles for Development of Challenging Drug Substance Stability-Indicating Methods by Yuill, Elizabeth M, Ileka, Kevin M, La Cruz, Thomas E, Li, Jieming, Shackman, Jonathan G, Tattersall, Peter I, Zang, Jia

“…Drug substance stability-indicating methods (SIMs) must undergo a litany of optimization and robustness stresses to ensure that the methods can be successfully…”
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Enantioselective Synthesis of a γ‑Secretase Modulator via Vinylogous Dynamic Kinetic Resolution by Strotman, Neil A, Ramirez, Antonio, Simmons, Eric M, Soltani, Omid, Parsons, Andrew T, Fan, Yu, Sawyer, James R, Rosner, Thorsten, Janey, Jacob M, Tran, Kristy, Li, Jun, La Cruz, Thomas E, Pathirana, Charles, Ng, Alicia T, Deerberg, Joerg

“…Two efficient asymmetric routes to γ-secretase modulator BMS-932481, under investigation for Alzheimer’s disease, have been developed. The key step for the…”
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A photochemical kinetic model for solid dosage forms by Carvalho, Thiago C., La Cruz, Thomas E., Tábora, Jose E.

“…[Display omitted] Photochemical kinetic models to describe the solution phase degradation of pharmaceutical compounds have been extensively reported, but…”
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Process Development and Scale-up of a Multicomponent Synthesis of a 3‑Methyl-1-aryl-1,2,4-triazole Building Block by La Cruz, Thomas E, Treitler, Daniel S, Tam, Annie, Smith, Kristine M, Leung, Simon, Pathirana, Charles, Peddicord, Michael, Fan, Yu, Vanyo, Dale, Deerberg, Joerg

“…The classical preparation of 3-methyl-1-aryl-1,2,4-triazoles through an SNAr reaction pathway results in a mixture of N-regioisomers. Removal of the unwanted…”
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Synthesis of the Spirofungin B Core by a Reductive Cyclization Strategy by La Cruz, Thomas E, Rychnovsky, Scott D

“…A reductive decyanation approach to the synthesis of the core of spirofungin B has been developed. Spirofungin B has only one anomeric stabilization in the…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 2. Strategic Selections in the Transition from an Enabling Route to a Commercial Synthesis by Chen, Ke, Risatti, Christina, Simpson, James, Soumeillant, Maxime, Soltani, Michelle, Bultman, Michael, Zheng, Bin, Mudryk, Boguslaw, Tripp, Jonathan C, La Cruz, Thomas E, Hsiao, Yi, Conlon, David A, Eastgate, Martin D

“…During the process of developing a synthesis to a complex molecule, multiple decisions are made regarding the strategies and tactics used to prepare key bonds…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 6. Friedel–Crafts Acylation/Hydrolysis and Amidation by Zheng, Bin, Silverman, Steven M, Steinhardt, Sarah E, Kolotuchin, Sergei, Iyer, Vidya, Fan, Junying, Skliar, Dimitri, McLeod, Douglas D, Bultman, Michael, Tripp, Jonathan C, Murugesan, Saravanababu, La Cruz, Thomas E, Sweeney, Jason T, Eastgate, Martin D, Conlon, David A

“…The development of a process for appending the oxalyl amide side chain to the azaindole core of the HIV-attachment inhibitor BMS-663068 is described. A…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 1. Evolution of Enabling Strategies by Fox, Richard J, Tripp, Jonathan C, Schultz, Mitchell J, Payack, Joseph F, Fanfair, Dayne D, Mudryk, Boguslaw M, Murugesan, Saravanababu, Chen, Chung-Pin H, La Cruz, Thomas E, Ivy, Sabrina E, Broxer, Sévrine, Cullen, Ryan, Erdemir, Deniz, Geng, Peng, Xu, Zhongmin, Fritz, Alan, Doubleday, Wendel W, Conlon, David A

“…The development of two enabling routes that led to the production of >1000 kg of BMS-663068 (3) is described. The route identified for the initial 100 kg…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 4. Synthesis of the 6‑Azaindole Core by Bultman, Michael S, Fan, Junying, Fanfair, Dayne, Soltani, Michelle, Simpson, James, Murugesan, Saravanababu, Soumeillant, Maxime, Chen, Ke, Risatti, Christina, La Cruz, Thomas E, Buono, Frederic G, Hung, Victor, Schild, Richard L, Ivy, Sabrina, Sweeney, Jason T, Conlon, David A, Eastgate, Martin D

“…We report research focused on the construction of the 6-azaindole core, a key intermediate in the synthesis of the clinical candidate BMS-663068. The work…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 8. Installation of the Phosphonoxymethyl Prodrug Moiety by Fox, Richard J, Cohen, Benjamin, La Cruz, Thomas E, Simpson, James H, Freitag, Adam, Saurer, Eric, Tripp, Jonathan C, Chen, Chien-Kuang, Beutner, Gregory L, Rosso, Victor W, Borgeson, Elizabeth, Glace, Andrew W, Eastgate, Martin D, Schild, Richard L, Sweeney, Jason T, Conlon, David A

“…The reaction optimization of an alkylation to enable the production of the penultimate intermediate of an HIV-attachment inhibitor candidate is described. To…”
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Preparation of the HIV Attachment Inhibitor BMS-663068. Part 9. Active Pharmaceutical Ingredient Process Development and Powder Properties by La Cruz, Thomas E, Saurer, Eric M, Engstrom, Joshua, Bultman, Michael S, Forest, Robert, Akpinar, Fulya, Ferreira, Glenn, Ho, Jeanne W, Huang, Masano, Soltani, Michelle, Murugesan, Saravanababu, Fanfair, Dayne, Ramirez, Antonio, Rosso, Victor W, Erdemir, Deniz, Rosenbaum, Tamar, Haslam, Michelle, Grier, Stephen, Peddicord, Michael, Pathirana, Charles, Marshall, Jonathan, Ding, Wei, Huang, Yande, Ayers, Sloan, Braem, Alan, Schild, Richard L, Ivy, Sabrina E, Payack, Joseph, McLeod, Douglas D, Nikitczuk, Whitney, Doubleday, Wendel, Shah, Sapna, Conlon, David A

“…This final communication, of a nine part publication series, details the process development history for the final synthetic step to prepare the drug substance…”
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A Reductive Cyclization Approach to Attenol A by La Cruz, Thomas E, Rychnovsky, Scott D

“…A reductive cyclization strategy was applied to the synthesis of attenol A. This nontraditional approach to the spiroacetal structure illustrated several…”
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Stereoselectivity of Intramolecular SN‘ Cyclizations of Alkyllithium Reagents on Methoxy Alkenes by La Cruz, Thomas E, Rychnovsky, Scott D

“…The cyclization of alkyllithium reagents onto methoxy alkenes has been investigated. The alkyllithium reagent was generated by reductive lithiation of an alkyl…”
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An azirine solid-state photodegradant of the CCR2/CCR5 dual antagonist BMS-813160 by Ayers, Sloan, La Cruz, Thomas, Park, Hyunsoo, Ramirez, Antonio, Hritzko, Benjamin, Sarjeant, Amy, Lin, Ziqing, Zaretsky, Serge, Huang, Yande, Zang, Jia, Yuill, Elizabeth M., Fenster, Michaël D.B.

“…[Display omitted] The synthesis of the CCR2/5 dual chemokine antagonist BMS-813160 (1) presented a number of interesting impurity and degradant structure…”
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Stereoselectivity of Intramolecular S N ‘ Cyclizations of Alkyllithium Reagents on Methoxy Alkenes by La Cruz, Thomas E., Rychnovsky, Scott D.

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Living in the Outskirts by De La Cruz, Thomas

“…Living in the Outskirts is a bildungsroman collection of short stories of a young Chicano growing up in the Rio Grande Valley town of Elsa, Texas. In the…”
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