MiniBlock and MiniBlock XT Configured to Suit Your Needs

Transcription

1 Minilock and Minilock XT onfigured to Suit Your eeds Minilock Set Quantity Package Quantity Minilock Synthesizer Shaking and Washing Station 1 ompact 1 igh apacity eat Transfer lock Vacuum ollection ase 1 Tall Tube xtender ecirculator Manifold 1 (-position) 1 (-position) ounterweight for Shaking Station 1 ir Push ssist evice 1 1 Inerting/Purging Manifold - Transfer dapter - esin ispenser - 1 onsumables Kit Small Large Minilock XT Set Quantity Package Quantity Inerting/Purging Manifold 1 eactor rame 1 emovable Vessel ack 1 efluxing Layer 1 Vessel ack emoval Tool 1 Sealing askets Inner/Piercing Septa Top Plate 1 Multi-layer Septa, Pre-scored for Top Plate IK ot Plate Stirrer (11V/0z 1 1 or V/0z Stir ars * * eaction Vessels * * *pplicable eaction Vessels and Stir ars Included or more information Mettler-Toledo utohem, Inc. 707 Samuel Morse rive olumbia, M US Tel: ax: mail: autochem@mt.com Subject to Technical hanges /00

2 Synthesis and Screening Minilock lexible fficient ompatible Maximize Productivity Maximize Prod with Parallel Synthesis

3 Minilock Synthetic hemists Your hoice for Synthesis Solution Phase Synthesis Solid Phase Synthesis Peptide Synthesis Parallel Purification Minilock The Minilock is a flexible, easy-to-use tool that maximizes productivity for synthetic chemists. Minilock is the only compact parallel synthesizer that enables synthesis via solid or solution phase as well as purification to be carried out on the same platform. Inert onditions ontinuous inert gas flow enables air/moisture sensitive reactions. asily add reagents through the septum layer. Today more chemists choose Minilock to increase productivity than any other similar tool. riginally designed by chemists at ristol-myers Squibb ompany, the Minilock has been further developed by MTTL TL to address a wide range of chemistry methodologies. Since using Minilocks, our labs report a 00% increase in new drug candidates and a 0% reduction in development time. Minilock is so widely accepted by our medicinal chemists that 70% of all current programs now use high throughput chemistry. r. arold Weller, esearch ellow ristol-myers Squibb gitation and esin Washing ustomized two- and six-position shakers result in precision vortex mixing of reactions. uilt-in washing capability enables rapid preparation of resins or efficient washing of products while reaction blocks remain on the shaker. eating and ooling Modular heat transfer jackets facilitate precision heating to and cooling down to -0.Temperature uniformity and reproducibility is within 1 at 0.

4 ne Platforn lexibility ed and blue Minilock combine to produce 9 compounds mL Vessels mL 1 Vessels ml 0 0 Vessels ml Vessels ml Vessels onfigure Minilock to Suit Your eeds Minilock can synthesize compounds in individual vessels ranging in size from as small as ml up to as large as 0ml - all delivered into racks with microplate footprints. This flexibility provides a smooth, seamless workflow from synthesis to screening With the Turn of a Key, collect products from Minilock cleanly and efficiently. Unique uilt-in Valve Provides rapid bottom filtration - no need to invert or disassemble the reactor. Saves time and prevents cross contamination. 3

5 Minilock XT Ultimate lexibility ne Platform our Volumes Parallel Synthesis eaction Screening atalyst Screening eflux and Inerting Minilock XT The Minilock XT is an easy to use reaction block designed for synthesis and screening reactions. pplications include synthesis of small organic molecules, optimization of critical process parameters, and screening for optimal reaction conditions. The Minilock XT is widely used by chemists working in biopharma, chemical, petrochemical, and polymers. The Minilock XT has a flexible and modular design that fits easily into your workflow, and is ideal for applications supported by statistical design of experiments (o). Minilock XT enables reactions to be run under stringent conditions allowing complete freedom to choose a synthetic route. lso designed by the discovery and development team at ristol-myers Squibb, the Minilock XT has been further developed and enhanced by MTTL TL to be compatible with the Minilock product line. Minilock performance has been outstanding even under the most stringent reaction conditions. Many of these require completely inert and anhydrous conditions at temperatures as low as -70. Prof. ieter nders, ead of the Institute of rganic hemistry, achen University of Technology (WT), ermany Inert onditions ontinuous inert gas flow enables air/moisture sensitive reactions. asily add reagents through the septum layer ml Vessels ml 1 Vessels ml Vessels 3mL Vessels onfigure Minilock XT to Suit Your eeds asily configure the Minilock XT to the scale.0 and number of experiments.0.0 based on project requirements

6 fficient eflux Single reflux jacket cools all vessels. o need for individual condensers. ittings provide quick and easy connection to your cooling liquid. Solvent loss on average is only 0.% per hour. Precise Temperature ontrol ontroller displays temperature and regulates heating. Working temperature range: -70 (with ice bath) to 10. Modular acks eadily interchangeable reaction vessel racks enable simple conversion between, 1,, and position arrays. The and position vessel racks are compatible with parallel centrifugal evaporators. asy eaction Setup single septum seals all vessels with a single layer and allows easy access to reactions.

7 hemistry pplications pplication Solutions 1 eactions cylation lkylation iaryl coupling iels-lder reaction eagents cid chlorides lkyl halides mines oranes nolate formation rignard reaction eck reaction eterocycle formation orohydrides rignard reagents Tetrakis MS for more application information Parallel Purification Minilock is ideal for post-synthesis cleanup using solid phase extraction (SP), solid liquid extraction (SL), and resin capture. This is achieved by transferring reaction products from the synthesis block to a second Minilock containing pre-loaded cartridges, or by passing through an SP filter plate. SP Purification Using nion xchange and 1 In the following example, nion xchange was used to remove by-products. The final product was then retained on 1. parallel purifications were carried out in just 1 minutes. ther sorbents investigated include SX, iatomaceous arth and Silica el. 1. I, amino acid. (remove silyl) 3. queous work-up. SX SX retains by-products a retains product Salts are eluted with water Product is eluted with Source: M. Young,.Weller, J. oberge and W. uediger, ISL 9, oston, M, 1-1 ct Metallation eduction eductive amination Saponification ydroxides Isocynates L Lil Sulfonylation Stille reaction Snr Suzuki coupling Mercaptans nuli T Q Solid Phase Synthesis The Minilock has fritted reaction vessels and combined with its patented built-in valve make solid phase synthesis easy and elegant: tedious resin washing steps can be performed by simply opening/ closing the valve in order to remove and add solvents. Vortex mixing ensures thorough agitation of resins. Synthesis of innoline erivatives: The icher-leavage In this example, the reaction required precision heating at 0, followed by a cleavage step, which included additional diversity elements in the cleavage cocktail. The same authors reported a series of novel amidation reactions requiring completely inert conditions, resulting in >9% yields. Ph l X X = r, I; Y=l, ' Pd(c), t 3 M, 0 o, 1h Y Ph Me 3 Si Y, acetone/ >0% Source: S. rase, S. ahmen, J. euts, Tetrahedron Left. 1999, 0, r Ph S Me 3 ' Y 11 Y ' Y n

8 Solution Phase Synthesis Minilock XT is extremely useful for complex, multistep synthesis protocols in a variety of reaction conditions. Ideal for reactions run at reflux and under inert conditions, Minilock XT uses a flexible reactor. The result - Minilock XT handles multiple-step synthesis protocols that require a wide range of reaction scales and arrays. Solution-Phase Parallel Synthesis of exahydro-1-isoindolone Libraries In this example, parallel solution phase synthesis of a series of libraries involving the synthesis of hexahydro- 1-isoindolones was performed exploiting a novel tactical combination of u-catalyzed three-component coupling and iels lder reactions. Three distinct libraries consisting of, 0, and 3 members were constructed. dditional sub-libraries of isoindolone scaffolds were prepared in a one-pot/two-step process and further diversified via Pd-catalyzed Suzuki crosscoupling reactions with boronic acids at two different diversification points. Snu 1 3 n u-catalysis + l n Libraries I-III (11 ompounds) Source: Zhang, Lushington, euenswander, ershberger, and Malinakova. J. omb. hem., (), -, 00. University of Kansas epartment of hemistry, enter for hemical Methodologies and Library evelopment. α-lkylation of SMP-ydrazones eactions can be carried out in round bottom or fritted vessels in a variety sizes. Purification and cleanup are simple: fritted reaction vessels, combined with the unique built-in valve, allow reaction products to be passed through scavenging resins in seconds. The following SMP reaction required strictly anhydrous conditions at -70 in the presence of corrosive reagents. The reactions were successfully carried out using Minilock fitted with inert atmosphere manifolds. The investigators repeated this reaction sequence in solid phase using a novel SMP resin, resulting in comparable yields. xpand Your apabilities Minilock ccessories Minilock XT ccessories Parallel Purification Minilock is ideal for postsynthesis cleanup using Solid Phase xtraction (SP) and techniques involving scavenger resins. pplications include removal of excess reagents and reactants, scavenging of metals, and removal of catalysts. esin ispensing esin loading is made simple with the Minilock resin dispenser. Pre-determined amounts of resins and powders are delivered to all the desired reaction positions in seconds, saving time and reducing errors. Parallel vaporation Microtiter plate design enables compatibility with commercially available parallel evaporation systems and eliminates the need for reformatting. Minilock XT Plus nables heating and cooling with common laboratory recirculators for chemists who desire more elaborate temperature control. eating or cooling liquid circulates through the XT frame and conducts to the reaction vessel rack. Low Temperature ath fficiently cool Minilock using a solvent/dry ice mixture. Insulated ice bath maintains dry ice/acetone mixture up to four hours lectrophiles (-X) tested I r 3 1. L, 0. X, -70 Source: Prof.. nders, J. Koebberling WT achen, ermany. I l 3 onc. xalic cid/m S X S Purity -90% rbital Shaking Minilock shaking stations allow controlled agitation of reactions using vigorous vortex mixing. uiltin washing capability permits rapid addition and removal of solvents for resin washing steps. eating and cooling is enabled via a recirculator manifold. 7