HA6973 Dihydroartemisinic Acid Powder (CAS No. 85031-59-0)

Dihydroartemisinic Acid Powder Description

Dihydroartemisinic Acid Powder appears as a white to off-white crystalline solid and exhibits a detectable herbal odour. Its molecular structure consists of a saturated decalin ring system with a carboxylic acid group at C-12 and an unsaturated side chain terminating in a methyl group. The compound melts between 138–141 °C and decomposes above 220 °C without boiling. It shows low solubility in water. It dissolves in polar organic solvents such as methanol, ethanol, acetone and dimethyl sulfoxide, and it is insoluble in non-polar solvents such as hexane. Crystalline analysis reveals a monoclinic lattice system stabilised by intermolecular hydrogen bonding. The powder is light sensitive and undergoes rapid oxidation when exposed to air or ultraviolet radiation; consequently, it shows gradual yellowing and degradation. Infrared spectroscopy detects absorption bands for carbonyl stretching near 1690 cm⁻¹, carboxylic hydroxyl vibrations around 3200 cm⁻¹ and alkene bonds at 1630 cm⁻¹. Ultraviolet spectroscopy shows a maximum absorption at 210 nanometres. Thermal gravimetric analysis indicates that weight loss initiates near 150 °C. The powder remains stable when stored under inert gas at low temperatures; however, it develops colour changes at room temperature due to oxidation. Its zwitterionic nature permits salt formation with bases, and the exocyclic double bond offers reactive sites for chemical modification. Particle morphology is typically in the form of fine needles, with a bulk density of approximately 0.55 grammes per cubic centimetre.

Dihydroartemisinic Acid Powder Applications

• Pharmaceutical Industry: Dihydroartemisinic acid acts as the biosynthetic precursor for semi‐synthetic production of artemisinin, the frontline antimalarial drug. It supports fermentation‐based processes that replace plant extraction. This change addresses supply challenges.
• Industrial Biotechnology: Engineered Saccharomyces cerevisiae strains utilise dihydroartemisinic acid as an intermediate in metabolic pathways to produce artemisinin at high yields. Fermentation processes have achieved a titre of 3.97 g/L in a 5‑L bioreactor, thereby reducing production costs.
• Agricultural and Botanical Research: Researchers use dihydroartemisinic acid to upregulate key artemisinin biosynthesis genes (e.g., ADS, CYP71AV1) in Artemisia annua. This procedure increases plant‐derived artemisinin yields and supports genetic engineering of high‐potency cultivars.
• Biochemical Research and Development: The compound is used as a reference standard to elucidate artemisinin biosynthesis mechanisms and enzyme kinetics. It is employed in studies of dehydrogenases such as AaDHAADH that catalyse its bidirectional conversion with artemisinic acid.
• Plant Metabolic Engineering: Transient expression systems in Nicotiana benthamiana use dihydroartemisinic acid to reconstruct artemisinin biosynthetic pathways. This method validates enzyme functions and optimises metabolic flux for plant‐based antimalarial production.

Dihydroartemisinic Acid Powder Packaging

Our products are packaged in customised cartons of various sizes according to the material dimensions. Small items are packed in PP boxes, while larger items are placed in custom wooden crates. We adhere to packaging customisation and use appropriate cushioning materials to maintain protection during transportation.

Packaging: Carton, Wooden Box, or Customised.

Please review the packaging details provided for your reference.

Manufacturing Process

1.       Testing Method

(1)    Chemical Composition Analysis – The composition is verified using techniques such as GDMS or XRF to ensure compliance with purity requirements.

(2)    Mechanical Properties Testing – This test includes measurements of tensile strength, yield strength and elongation to assess material performance.

(3)    Dimensional Inspection – Thickness, width and length are measured to confirm adherence to specified tolerances.

(4)    Surface Quality Inspection – Defects such as scratches, cracks or inclusions are checked by visual and ultrasonic examination.

(5)    Hardness Testing – Material hardness is determined to confirm uniformity and mechanical reliability.

Please refer to the SAM testing procedures for detailed information.

Dihydroartemisinic Acid Powder FAQs

Q1. How to resolve inconsistent particle size during scale-up crystallisation?

Uniform crystals (D90 ≈150 µm) are achieved by applying a controlled cooling profile. The material is held at 40 °C for 2 hours, cooled to 25 °C over 2 hours and then cooled to 4 °C for 5 hours. The addition of 0.5% w/w colloidal silica (Aerosil 200) prevents agglomeration and improves powder flowability by 35% in Carr index tests.

Q2. How to handle temperature excursions during shipping (e.g., 15 °C vs required -20 °C)?

Peroxide levels should be tested immediately using EP strips. Batches exceeding 50 ppm must be rejected. If chiral purity drops by more than 0.3%, the batch is reclassified for non-critical use after adding 0.2% BHT and repackaging under nitrogen.

Q3. How to control crystal morphology during large-scale crystallisation?

A multi-stage cooling protocol is implemented (cooling from 40 °C to 25 °C over 2 hours, then to 4 °C for 5 hours) with a 0.5% w/w colloidal silica additive to obtain a consistent D90 particle size of 150 ± 30 µm. Seeding at 35 °C using 0.1% pre-isomorphic crystals further improves monodispersity and reduces Carr index variability by 40% in 500 kg batches.

Related Information

Common Preparation Methods

Dihydroartemisinic acid synthesis begins with dissolving artemisinin in THF (0.5 M) under a nitrogen atmosphere. Sodium borohydride (1.2 equivalents) is added at temperatures maintained below 10 °C, followed by the addition of cobalt(II) chloride catalyst (0.05 equiv). The mixture is stirred at 25 °C for 3 hours until over 98% conversion is achieved, and then it is oxidised with manganese dioxide (3.0 equiv) in toluene at 35 °C for 8 hours, yielding 95–97% crude product. Purification involves acid removal via a 10% sodium bicarbonate wash, metal reduction to below 1 ppm using Chelex-100 resin at a pH of 6.2, and crystallisation from an acetonitrile/water solvent system (4:1 v/v) with 0.5% colloidal silica under controlled cooling from 40 °C to 4 °C over 7 hours. The crystals are washed with an n-heptane/toluene mixture (7:3 v/v) to reduce dimeric impurities to below 0.15% and are then rotary-dried at 65 °C under nitrogen with the addition of 0.1% BHT antioxidant. The procedure yields a white crystalline product (D90 = 150 ± 30 µm) with a purity exceeding 99.5% and residual solvents below 300 ppm.